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Cytoskeleton
The cytoskeleton is a filamentous network of F-actin microtubules and intermediate filaments (IFs) composed of one of threechemically distinct subunits actin tubulin or one of several classes of IF protein Cytoskeleton not only helps cells maintain theirshape and internal organization but also provides mechanical support that enables cells to carry out essential functions likedivision and movement
The cytoskeleton is involved in intracellular signal transduction at least two ways First individual proteins of the cytoskeleton mightparticipate directly in signal transduction by linking two or more signaling proteins Second the cytoskeleton might provide amacromolecular scaffold which spatially organizes components of a signal transduction cascade Cell migration is a complex andmultistep process involved in homeostasis maintenance morphogenesis and disease development such as cancer metastasis andrequires coordination of cytoskeletal dynamics and reorganization cell adhesion and signal transduction and takes a variety offorms Many signaling pathways including Rho-family GTPases PaxillinFAK signaling and PI3K signaling is involved in the processby regulating cytoskeletal activity
Since the cytoskeleton is involved in virtually all cellular processes abnormalities in this essential cellular component frequentlyresult in disease Drugs that modulate microtubule stability inhibitors of posttranslational modifications of cytoskeletalcomponents specifically compounds affecting the levels of tubulin acetylation and compounds targeting signaling moleculeswhich regulate cytoskeleton dynamics constitute the mostly addressed therapeutic interventions for the diseases including cancerand neurodegenerative disorders
References[1] Janmey PA Physiol Rev 1998 Jul78(3)763-81[2] Forgacs G et al J Cell Sci 2004 Jun 1117(Pt 13)2769-75[3] Eira J et al Prog Neurobiol 2016 Jun14161-82
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bull Arp23 Complex 3
bull Dynamin 6
bull Gap Junction Protein 8
bull Integrin 11
bull Kinesin 20
bull MicrotubuleTubulin 23
bull Mps1 39
bull Myosin 42
bull PAK 45
bull ROCK 48
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Target List in Cytoskeleton
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Arp23 ComplexActin-related protein 23 complex
The intact ARP23 complex is first purified from based on its affinity for the actin-binding protein profilinAcanthamoeba castellaniiand is shown to consist of a stable assembly of seven polypeptides Two of the subunits are actin-related proteins of the ARP2 andARP3 subfamilies giving the complex its name
The ARP23 complex possesses little biochemical activity on its own However when engaged by nucleation-promoting factor (NPF)proteins it is activated to initiate the formation of a new (daughter) filament that emerges from an existing (mother) filament in ay-branch configuration with a regular 70deg branch angle This coupling of nucleation and branching by the ARP23 complex isreferred to as autocatalytic branching or dendritic nucleation and is central to its functions in vivo
Polymerization of actin filaments directed by the Arp23 complex supports many types of cellular movements
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Arp23 Complex Inhibitors amp Activators
187-1 N-WASP inhibitorCat No HY-P1045
187-1 N-WASP inhibitor a 14-aa cyclic peptideis an allosteric neural Wiskott-Aldrich syndrome
inhibitor 187-1 N-WASPprotein (N-WASP)inhibitor potently inhibits actin assembly inducedby phosphatidylinositol 45-bisphosphate (PIP2)with an of 2 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
187-1 N-WASP inhibitor TFACat No HY-P1045A
187-1 N-WASP inhibitor TFA a 14-aa cyclicpeptide is an allosteric neural Wiskott-Aldrich
inhibitorsyndrome protein (N-WASP)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Benproperine phosphateCat No HY-114657A
Benproperine phosphate is an orally active potentactin-related protein 23 complex subunit 2
inhibitor Benproperine phosphate(ARPC2)attenuates the actin polymerization rate of actionpolymerization nucleation by impairing Arp23function
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
CK-636 (CK-0944636) Cat No HY-15892
CK-636 is a cell permeable inhibitor of Arp23 that could inhibit actincomplex
polymerization with values of 4 μM 24 μMIC50
and 32 μM for human fission yeast and bovinerespectively
Purity 9843Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
CK-666Cat No HY-16926
CK-666 is a cell-permeable actin-related protein inhibitor ( =12 μM) CK-666Arp23 complex IC50
binds to Arp23 complex stabilizes the inactivestate of the complex blocking movement of theArp2 and Arp3 subunits into the activatedfilament-like (short pitch) conformation
Purity 9963Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
CK-869Cat No HY-16927
CK-869 is an Actin-Related Protein 23 (ARP23)complex inhibitor with an of 7 μMIC50
Purity 9976Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Cytochalasin B (Phomin) Cat No HY-16928
Cytochalasin B is a cell-permeable mycotoxinbinding to the barbed end of filamentsactindisrupting the formation of actin polymers with
value of 14-22 nM for F-actinKd
Purity 9892Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Cytochalasin D (Zygosporin A NSC 209835) Cat No HY-N6682
Cytochalasin D (Zygosporin A NSC 209835) is apotent and cell-permeable inhibitor of actinpolymerization derived from fungus inhibits theG-actinndashcofilin interaction by binding to G-actin
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
Dihydrocytochalasin BCat No HY-N6701
Dihydrocytochalasin B (H2CB) is a Cytokinesisinhibitor and changes the morphology of the cellssimilar to that of cytochalasin B does notinhibit glucose transport
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
JasplakinolideCat No HY-P0027
Jasplakinolide is a potent actin polymerizationinducer and stabilizes pre-existing actinfilaments Jasplakinolide binds to F-actincompetitively with phalloidin with a of 15Kd
nM
Purity ge980Clinical Data No Development ReportedSize 100 μg
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Latrunculin A (LAT-A) Cat No HY-16929
Latrunculin A (LAT-A) is a toxin isolated from thered sea sponge binds toLatrunculia magnificaactin monomers inhibits polymerization of actinwith s of 01 04 47 μM and 019 μM forKd
ATP-actin ADP-Pi-actin ADP-actin and G-actinrespectively
Purity ge980Clinical Data No Development ReportedSize 100 μg
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Dynamin
Dynamins are large superfamily GTPase proteins that are involved in various cellular processes including budding of transportvesicles division of organelles cytokinesis and pathogen resistance Dynamins are involved in scission (cleavage of the vesicle fromthe parent membrane) of nascent vesicles from parent membranes in eukaryotic cells Dynamins interact directly with the lipidbilayer at the necks of clathrin-coated pits to sever and release coated vesicles Dynamins contain five domains including GTPasedomain middle domain PH domain GTPase effector domain (GED) and proline rich domain (PRD) while the dynamin-relatedproteins (DRPs) lack one or more of these domains or have additional domains Dynamins and DRPs participate in a wide variety ofcellular processes including budding mitochondrial fission (mammalian Dlp1 and Dnm1) and fusionSaccharomyces cerevisiae(mammalian OPA1 Mgm1 and Msp1) vacuolar fission ( Vps1)Scerevisiae Schizosaccharomycespombe S cerevisiaeinterferon-induced anti-viral protection (fish Mx proteins) plant cell cytokinesis and membrane fission ( DRPArabidopsis thalianaproteins) as well as pathogen resistance
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Dynamin Inhibitors
Dynamin inhibitory peptideCat No HY-P1083
Dynamin inhibitory peptide competitively blocksbinding of to amphiphysin thusdynaminpreventing endocytosis Dynamin inhibitory peptideblocks the dopamine D3 effect on GABAA receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Dynamin inhibitory peptide TFACat No HY-P1083A
Dynamin inhibitory peptide TFA competitivelyblocks binding of to amphiphysin thusdynaminpreventing endocytosis Dynamin inhibitory peptideTFA blocks the dopamine D effect on GABA3 A
receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynaMin inhibitory peptide myristoylatedCat No HY-P1369
DynaMin inhibitory peptide myristoylated is a inhibitor to interfere with the bindingDynaMin
of amphiphysin with dynamin DynaMin inhibitorypeptide myristoylated is a membrane-permeant formof the peptide that prevents endocytosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynaMin inhibitory peptide myristoylated TFACat No HY-P1369A
DynaMin inhibitory peptide myristoylated TFA is a inhibitor to interfere with the bindingDynaMin
of amphiphysin with dynamin DynaMin inhibitorypeptide myristoylated TFA is a membrane-permeantform of the peptide that prevents endocytosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynasoreCat No HY-15304
Dynasore is a cell-permeable inhibitordynaminwith an of 15 μMIC50
Purity 9870Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Hydroxy-Dynasore (Dyngo-4a) Cat No HY-13863
Hydroxy Dynasore (Dyngo-4a) a structural analogof Dynasore (HY-15304) is an potency improvedlow cytotoxicity and nonspecific binding
inhibitor with values of 038dynamin IC50
μM and 23 μM for brain dynamin I andrecombinant rat dynamin II respectively
Purity 9614Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Mdivi-1 (Mitochondrial division inhibitor 1) Cat No HY-15886
Mdivi-1 is a selective dynamin-related protein 1( ) inhibitor Mdivi-1 is a mitochondrialDrp1division inhibitormitophagy
Purity 9973Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SchaftosideCat No HY-N0703
Schaftoside is a flavonoid found in a variety ofChinese herbal medicines such as Eleusine indicaSchaftoside inhibits the expression of TLR4 andMyd88 Schaftoside also decreases Drp1 expressionand phosphorylation and reduces mitochondrialfission
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 20 mg
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Gap Junction Protein
Gap junction channels are essential in normal heart function and they assist in the mediated spread of electrical impulses thatstimulate synchronized contraction (via an electrical syncytium) of cardiac tissues
Gap junction (GJ) proteins play an important role in direct communication between cells of many tissue types GJs are specialisedintercellular membrane-spanning domains that allow the passage of small molecules including second messenger (eg c-AMPinositol triphosphate) or ionic signals from one cell to another GJ proteins and their long evolutionary history have permittedadaptation of gap junction intercellular communication (GJIC) with several important functions and multiple regulatory processesFormation of GJIC is an essential mechanism in coordinating growth and development and tissue compartmentalization duringembryonic development
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Gap Junction Protein Inhibitors amp Modulators
AT-1002Cat No HY-114426
AT-1002 a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AT-1002 TFACat No HY-114426A
AT-1002 TFA a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Carbenoxolone disodiumCat No HY-B1367
Carbenoxolone disodium is the active metaboliteof Glycyrrhizic acid (HY-N0184) and the inhibitorof human and bacterial 11β-HSD 3α 20β-HSDCarbenoxolone disodium is an uncoupling agent for
and a potent inhibitor of gap junctions Vacciniavirus replication
Purity 9929Clinical Data LaunchedSize 10 mM times 1 mL 25 mg 50 mg 100 mg
Danegaptide (GAP-134 ZP 1609) Cat No HY-10913
Danegaptide (GAP-134) is a potent selective andorally active modifier with angap-junctionantiarrhythmic effect
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
Danegaptide Hydrochloride (GAP-134 Hydrochloride ZP 1609 Hydrochloride) Cat No HY-10913A
Danegaptide Hydrochloride (GAP-134 Hydrochloride)is a potent selective and orally active
modifier with an antiarrhythmicgap-junctioneffect
Purity 9975Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Gap 26Cat No HY-P1082
Gap 26 is a connexin mimetic peptide composed ofresidue numbers 63-75 of the first extracellularloop of connexin 43 (gap junction blocker)containing the SHVR amino acid motif
Purity 9964Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 26 TFACat No HY-P1082A
Gap 26 TFA is a connexin mimetic peptide composedof residue numbers 63-75 of the firstextracellular loop of connexin 43 (gap junctionblocker) containing the SHVR amino acid motif
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 27Cat No HY-P0139
Gap 27 a synthetic connexin43 mimetic peptide isa gap junction inhibitor Gap 27 possessesconserved sequence homology to a portion of thesecond extracellular loop leading into the fourthtransmembrane connexin segment
Purity 9807Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19Cat No HY-P1136
Gap19 a peptide derived from nine amino acids ofthe Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19 TFACat No HY-P1136A
Gap19 TFA a peptide derived from nine amino acidsof the Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 TFA inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
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Larazotide acetateCat No HY-106268A
Larazotide acetate is a synthetic peptideLarazotide acetate acts as a tight junctionregulator and reverses leaky junctions to theirnormally closed state
Purity 9968Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Meclofenamate sodium (Meclofenamic acid sodium) Cat No HY-B1320
Meclofenamic acid sodium is a nonsteroidalanti-inflammatory drug (NSAID) approved for use inarthritis (osteo and rheumatoid) analgesia (mildto moderate pain) dysmenorrhea and heavymenstrual blood loss (menorrhagia)
Purity 9862Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 200 mg
Meclofenamic acidCat No HY-117275
Meclofenamic Acid a non-steroidalanti-inflammatory agent is a highly selectivefat mass and obesity-associated (FTO) enzymeinhibitor Meclofenamic Acid competes with FTObinding for the m(6)A-containing nucleic acid
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Rotigaptide (ZP123) Cat No HY-106225
Rotigaptide (ZP123) is a novel and specificmodulator of Rotigaptideconnexin 43 (Cx43)prevents the uncoupling of Cx43-mediated gap
communication and normalizes cell-to-celljunctioncommunication during acute metabolic stress
Purity 9963Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg
TAT-Gap19Cat No HY-P1136B
TAT-Gap19 a Cx mimetic peptide is a specific inhibitorconnexin43 hemichannel (Cx43 HC)
TAT-Gap19 does not inhibits the corresponding Cx43GJCs TAT-Gap19 traverses the blood-brain barrierand alleviate liver fibrosis in mice
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tonabersat (SB-220453) Cat No HY-15204
Tonabersat (SB-220453) is a modulatorgap-junctionTonabersat prevents inflammatory damage in thecentral nervous system
Purity 9968Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
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Integrin
Integrins a family of heterodimeric adhesion receptors for diverse extracellular matrices have consistently been implicated ascrucial drivers of ovarian cancer development and progression A number of the RGD-based members of the integrin familyincluding α5β1 and αvβ3 or αvβ5 integrins are markedly elevated in aggressive ovarian tumors These adhesion receptors appearto promote cell adhesion survival motility and invasion during ovarian tumor growth or metastatic progression Importantly thefunctions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signalingincluding the PI3KAkt- and RasMAPK-dependent pathways
Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion Modulationof these molecules particularly αv integrin family has exhibited profound effects on fibrosis in multiple organ and disease stateBased on the several studies the integrins αvβ3 αvβ5 αvβ6 and αvβ8 have been known to modulate the fibrotic process viaactivation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis
Each integrin is typically formed by the non-covalent pairing of one α subunit of which 18 types are known to exist and one βsubunit of which 8 types are known to exist Together 24 distinct heterodimers have been identified to date The αv subunit canform heterodimers with the β1 β3 β5 β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11 andαv indicating that not all theoretically possible α and subunit pairs form Interestingly the activation of TGF-β appears to be acommon function of multiple αv integrins
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Integrin Inhibitors Agonists Antagonists amp Modulators
A-205804Cat No HY-100226
A-205804 is an orally bioavailable potent andselective lead inhibitor of andE-selectin
expression with an of 20 nM and 25ICAM-1 IC50
nM for E-selectin and ICAM-1 respectivelyA-205804 can be used in the research of chronicinflammatory diseases
Purity 9812Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Arg-Gly-Asp-Ser (RGDS peptide Fibronectin tetrapeptide) Cat No HY-12290
Arg-Gly-Asp-Ser is an integrin binding sequencethat inhibits functionintegrin receptordecreases systemic inflammation via inhibition ofcollagen-triggered activation of leukocytes andattenuates expression of inflammatory cytokinesiNOS and MMP-9
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Arg-Gly-Asp-Ser (TFA) (RGDS peptide (TFA) Fibronectin tetrapeptide (TFA)) Cat No HY-12290A
Arg-Gly-Asp-Ser (TFA) is an integrin bindingsequence that inhibits functionintegrin receptorArg-Gly-Asp-Ser (TFA) directly and specificallybind pro-caspase-8 pro-caspase-9 andpro-caspase-3 while it does not bindpro-caspase-1
Purity gt98Clinical DataSize 1 mg 5 mg
ATN-161 trifluoroacetate salt (ATN-161 TFA salt) Cat No HY-13535A
ATN-161 trifluoroacetate salt is a novel integrin antagonist which inhibits angiogenesis andα5β1
growth of liver metastases in a murine model
Purity ge950Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg
BI-1950Cat No HY-124040
BI-1950 is a highly potent lymphocyte function inhibitor LFA-1 isassociated antigen-1 (LFA-1)
an essential component in normal immune systemfunction and a target for drug discovery
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO-1211Cat No HY-14126
BIO-1211 is a highly selective and orally active inhibitor with values of 4 nMα4β1 (VLA-4) IC50
and 2 μM for α4β1 and α4β7 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192Cat No HY-107589
BIO5192 is a selective and potent integrin α4β1(VLA-4) inhibitor ( lt10 pM) BIO5192Kd
selectively binds to α4β1 ( =18 nM) over aIC50
range of other integrins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192 hydrateCat No HY-107589A
BIO5192 hydrate is a selective and potent integrin inhibitor ( lt10 pM) BIO5192α4β1 (VLA-4) Kd
hydrate selectively binds to α4β1 ( =18 nM)IC50
over a range of other integrins
Purity ge980Clinical Data No Development ReportedSize 1 mg
BMS-688521Cat No HY-10596
BMS-688521 is a highly potent orally activeinhibitor of the interaction withLFA-1ICAMan of 25 nM in the adhesion assay and anIC50
of 60 nM in the MLR assay BMS-688521 isIC50
efficacious in a mouse allergic eosinophilic lunginflammation model
Purity 9925Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
BOP sodiumCat No HY-129453
BOP sodium is a potent and selective dual inhibitor with values inα9β1α4β1 integrin Kd
the picomolar range BOP sodium shows the rapidand preferential mobilization of hematopoieticstem cell (HSC) and progenitors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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c(phg-isoDGR-(NMe)k)Cat No HY-111413
c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
c(phg-isoDGR-(NMe)k) TFACat No HY-111413A
c(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
CarotegrastCat No HY-14857
Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor
activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Carotegrast methyl (AJM300) Cat No HY-124290
Carotegrast methyl (AJM300) is an orally activeand selective antagonist HCA2969 anα4 integrinactive metabolite of AJM300 is a specific dualα4β1α4β7 integrin antagonist Carotegrast methylprevents the development of colitis in miceltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cilengitide (EMD 121974) Cat No HY-16141
Cilengitide (EMD 121974) is a potent and selectiveinhibitor of the and integrins α βν 3 α βν 5
Cilengitide inhibits binding of isolated α βν 3
and α β to Vitronectin with an IC value of 4ν 5 50
and 79 nM respectively
Purity 9932Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cilengitide TFA (EMD 121974 TFA) Cat No HY-16143
Cilengitide is a potent and selective integrininhibitor for α β and α β receptor withv 3 v 5
values of 4 nM and 79 nM respectivelyIC50
Purity 9885Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Cucurbitacin BCat No HY-N0416
Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids could represscancer cell progression
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
CWHM-12Cat No HY-18644
CWHM-12 is a potent inhibitor of withαV integrinss of 02 08 15 and 18 nM for IC50 αvβ8
and αvβ3 αvβ6 αvβ1
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK)Cat No HY-P0023
Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin with an of 094 nMα βv 3 IC50
Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK) TFACat No HY-P0023A
Cyclo(-RGDfK) TFA is a potent and selectiveinhibitor of the integrin with an ofα βv 3 IC50
094 nM Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity 9981Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
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Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat No HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof with antitumor activityintegrin αvβ3
Purity 9940Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RADfK)Cat No HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch therapy and diagnosis ofneoangiogenesis
Purity 9803Clinical Data No Development ReportedSize 1 mg
Cyclo(RGDyK)Cat No HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nMintegrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RGDyK) trifluoroacetateCat No HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
E7820 (ER68203-00) Cat No HY-14571
E7820 (ER68203-00) an orally active aromaticsulfonamide derivative is a unique angiogenesisinhibitor suppressing an expression of integrin
subunit on endothelium E7820 inhibits ratalpha2aorta angiogenesis with an of 011 μgmlIC50
Purity 9936Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
EchistatinCat No HY-P1189
Echistatin the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Echistatin TFACat No HY-P1189A
Echistatin TFA the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EptifibatideCat No HY-B0686
Eptifibatide is a cyclic heptapeptide acts as acompetitive antagonist for the activated platelet
with anti-plateletglycoprotein IIbIIIa receptoractivity
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Eptifibatide acetateCat No HY-B0686A
Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Firategrast (SB 683699) Cat No HY-14951
Firategrast (SB 683699) is an orally active andspecific antagonistα4β1α4β7 integrinFirategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) anddecreases multiple sclerosis (MS) activity
Purity 9988Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
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ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
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SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
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Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
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AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
wwwMedChemExpresscom 25
BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
wwwMedChemExpresscom 27
DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 35
Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
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Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 51
ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
bull Arp23 Complex 3
bull Dynamin 6
bull Gap Junction Protein 8
bull Integrin 11
bull Kinesin 20
bull MicrotubuleTubulin 23
bull Mps1 39
bull Myosin 42
bull PAK 45
bull ROCK 48
Inhibitors Agonists Screening LibrarieswwwMedChemExpresscom
Target List in Cytoskeleton
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Arp23 ComplexActin-related protein 23 complex
The intact ARP23 complex is first purified from based on its affinity for the actin-binding protein profilinAcanthamoeba castellaniiand is shown to consist of a stable assembly of seven polypeptides Two of the subunits are actin-related proteins of the ARP2 andARP3 subfamilies giving the complex its name
The ARP23 complex possesses little biochemical activity on its own However when engaged by nucleation-promoting factor (NPF)proteins it is activated to initiate the formation of a new (daughter) filament that emerges from an existing (mother) filament in ay-branch configuration with a regular 70deg branch angle This coupling of nucleation and branching by the ARP23 complex isreferred to as autocatalytic branching or dendritic nucleation and is central to its functions in vivo
Polymerization of actin filaments directed by the Arp23 complex supports many types of cellular movements
wwwMedChemExpresscom 3
Arp23 Complex Inhibitors amp Activators
187-1 N-WASP inhibitorCat No HY-P1045
187-1 N-WASP inhibitor a 14-aa cyclic peptideis an allosteric neural Wiskott-Aldrich syndrome
inhibitor 187-1 N-WASPprotein (N-WASP)inhibitor potently inhibits actin assembly inducedby phosphatidylinositol 45-bisphosphate (PIP2)with an of 2 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
187-1 N-WASP inhibitor TFACat No HY-P1045A
187-1 N-WASP inhibitor TFA a 14-aa cyclicpeptide is an allosteric neural Wiskott-Aldrich
inhibitorsyndrome protein (N-WASP)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Benproperine phosphateCat No HY-114657A
Benproperine phosphate is an orally active potentactin-related protein 23 complex subunit 2
inhibitor Benproperine phosphate(ARPC2)attenuates the actin polymerization rate of actionpolymerization nucleation by impairing Arp23function
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
CK-636 (CK-0944636) Cat No HY-15892
CK-636 is a cell permeable inhibitor of Arp23 that could inhibit actincomplex
polymerization with values of 4 μM 24 μMIC50
and 32 μM for human fission yeast and bovinerespectively
Purity 9843Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
CK-666Cat No HY-16926
CK-666 is a cell-permeable actin-related protein inhibitor ( =12 μM) CK-666Arp23 complex IC50
binds to Arp23 complex stabilizes the inactivestate of the complex blocking movement of theArp2 and Arp3 subunits into the activatedfilament-like (short pitch) conformation
Purity 9963Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
CK-869Cat No HY-16927
CK-869 is an Actin-Related Protein 23 (ARP23)complex inhibitor with an of 7 μMIC50
Purity 9976Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Cytochalasin B (Phomin) Cat No HY-16928
Cytochalasin B is a cell-permeable mycotoxinbinding to the barbed end of filamentsactindisrupting the formation of actin polymers with
value of 14-22 nM for F-actinKd
Purity 9892Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Cytochalasin D (Zygosporin A NSC 209835) Cat No HY-N6682
Cytochalasin D (Zygosporin A NSC 209835) is apotent and cell-permeable inhibitor of actinpolymerization derived from fungus inhibits theG-actinndashcofilin interaction by binding to G-actin
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
Dihydrocytochalasin BCat No HY-N6701
Dihydrocytochalasin B (H2CB) is a Cytokinesisinhibitor and changes the morphology of the cellssimilar to that of cytochalasin B does notinhibit glucose transport
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
JasplakinolideCat No HY-P0027
Jasplakinolide is a potent actin polymerizationinducer and stabilizes pre-existing actinfilaments Jasplakinolide binds to F-actincompetitively with phalloidin with a of 15Kd
nM
Purity ge980Clinical Data No Development ReportedSize 100 μg
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Latrunculin A (LAT-A) Cat No HY-16929
Latrunculin A (LAT-A) is a toxin isolated from thered sea sponge binds toLatrunculia magnificaactin monomers inhibits polymerization of actinwith s of 01 04 47 μM and 019 μM forKd
ATP-actin ADP-Pi-actin ADP-actin and G-actinrespectively
Purity ge980Clinical Data No Development ReportedSize 100 μg
wwwMedChemExpresscom 5
Dynamin
Dynamins are large superfamily GTPase proteins that are involved in various cellular processes including budding of transportvesicles division of organelles cytokinesis and pathogen resistance Dynamins are involved in scission (cleavage of the vesicle fromthe parent membrane) of nascent vesicles from parent membranes in eukaryotic cells Dynamins interact directly with the lipidbilayer at the necks of clathrin-coated pits to sever and release coated vesicles Dynamins contain five domains including GTPasedomain middle domain PH domain GTPase effector domain (GED) and proline rich domain (PRD) while the dynamin-relatedproteins (DRPs) lack one or more of these domains or have additional domains Dynamins and DRPs participate in a wide variety ofcellular processes including budding mitochondrial fission (mammalian Dlp1 and Dnm1) and fusionSaccharomyces cerevisiae(mammalian OPA1 Mgm1 and Msp1) vacuolar fission ( Vps1)Scerevisiae Schizosaccharomycespombe S cerevisiaeinterferon-induced anti-viral protection (fish Mx proteins) plant cell cytokinesis and membrane fission ( DRPArabidopsis thalianaproteins) as well as pathogen resistance
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Dynamin Inhibitors
Dynamin inhibitory peptideCat No HY-P1083
Dynamin inhibitory peptide competitively blocksbinding of to amphiphysin thusdynaminpreventing endocytosis Dynamin inhibitory peptideblocks the dopamine D3 effect on GABAA receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Dynamin inhibitory peptide TFACat No HY-P1083A
Dynamin inhibitory peptide TFA competitivelyblocks binding of to amphiphysin thusdynaminpreventing endocytosis Dynamin inhibitory peptideTFA blocks the dopamine D effect on GABA3 A
receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynaMin inhibitory peptide myristoylatedCat No HY-P1369
DynaMin inhibitory peptide myristoylated is a inhibitor to interfere with the bindingDynaMin
of amphiphysin with dynamin DynaMin inhibitorypeptide myristoylated is a membrane-permeant formof the peptide that prevents endocytosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynaMin inhibitory peptide myristoylated TFACat No HY-P1369A
DynaMin inhibitory peptide myristoylated TFA is a inhibitor to interfere with the bindingDynaMin
of amphiphysin with dynamin DynaMin inhibitorypeptide myristoylated TFA is a membrane-permeantform of the peptide that prevents endocytosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynasoreCat No HY-15304
Dynasore is a cell-permeable inhibitordynaminwith an of 15 μMIC50
Purity 9870Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Hydroxy-Dynasore (Dyngo-4a) Cat No HY-13863
Hydroxy Dynasore (Dyngo-4a) a structural analogof Dynasore (HY-15304) is an potency improvedlow cytotoxicity and nonspecific binding
inhibitor with values of 038dynamin IC50
μM and 23 μM for brain dynamin I andrecombinant rat dynamin II respectively
Purity 9614Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Mdivi-1 (Mitochondrial division inhibitor 1) Cat No HY-15886
Mdivi-1 is a selective dynamin-related protein 1( ) inhibitor Mdivi-1 is a mitochondrialDrp1division inhibitormitophagy
Purity 9973Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SchaftosideCat No HY-N0703
Schaftoside is a flavonoid found in a variety ofChinese herbal medicines such as Eleusine indicaSchaftoside inhibits the expression of TLR4 andMyd88 Schaftoside also decreases Drp1 expressionand phosphorylation and reduces mitochondrialfission
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 20 mg
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Gap Junction Protein
Gap junction channels are essential in normal heart function and they assist in the mediated spread of electrical impulses thatstimulate synchronized contraction (via an electrical syncytium) of cardiac tissues
Gap junction (GJ) proteins play an important role in direct communication between cells of many tissue types GJs are specialisedintercellular membrane-spanning domains that allow the passage of small molecules including second messenger (eg c-AMPinositol triphosphate) or ionic signals from one cell to another GJ proteins and their long evolutionary history have permittedadaptation of gap junction intercellular communication (GJIC) with several important functions and multiple regulatory processesFormation of GJIC is an essential mechanism in coordinating growth and development and tissue compartmentalization duringembryonic development
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Gap Junction Protein Inhibitors amp Modulators
AT-1002Cat No HY-114426
AT-1002 a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AT-1002 TFACat No HY-114426A
AT-1002 TFA a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Carbenoxolone disodiumCat No HY-B1367
Carbenoxolone disodium is the active metaboliteof Glycyrrhizic acid (HY-N0184) and the inhibitorof human and bacterial 11β-HSD 3α 20β-HSDCarbenoxolone disodium is an uncoupling agent for
and a potent inhibitor of gap junctions Vacciniavirus replication
Purity 9929Clinical Data LaunchedSize 10 mM times 1 mL 25 mg 50 mg 100 mg
Danegaptide (GAP-134 ZP 1609) Cat No HY-10913
Danegaptide (GAP-134) is a potent selective andorally active modifier with angap-junctionantiarrhythmic effect
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
Danegaptide Hydrochloride (GAP-134 Hydrochloride ZP 1609 Hydrochloride) Cat No HY-10913A
Danegaptide Hydrochloride (GAP-134 Hydrochloride)is a potent selective and orally active
modifier with an antiarrhythmicgap-junctioneffect
Purity 9975Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Gap 26Cat No HY-P1082
Gap 26 is a connexin mimetic peptide composed ofresidue numbers 63-75 of the first extracellularloop of connexin 43 (gap junction blocker)containing the SHVR amino acid motif
Purity 9964Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 26 TFACat No HY-P1082A
Gap 26 TFA is a connexin mimetic peptide composedof residue numbers 63-75 of the firstextracellular loop of connexin 43 (gap junctionblocker) containing the SHVR amino acid motif
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 27Cat No HY-P0139
Gap 27 a synthetic connexin43 mimetic peptide isa gap junction inhibitor Gap 27 possessesconserved sequence homology to a portion of thesecond extracellular loop leading into the fourthtransmembrane connexin segment
Purity 9807Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19Cat No HY-P1136
Gap19 a peptide derived from nine amino acids ofthe Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19 TFACat No HY-P1136A
Gap19 TFA a peptide derived from nine amino acidsof the Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 TFA inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
wwwMedChemExpresscom 9
Larazotide acetateCat No HY-106268A
Larazotide acetate is a synthetic peptideLarazotide acetate acts as a tight junctionregulator and reverses leaky junctions to theirnormally closed state
Purity 9968Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Meclofenamate sodium (Meclofenamic acid sodium) Cat No HY-B1320
Meclofenamic acid sodium is a nonsteroidalanti-inflammatory drug (NSAID) approved for use inarthritis (osteo and rheumatoid) analgesia (mildto moderate pain) dysmenorrhea and heavymenstrual blood loss (menorrhagia)
Purity 9862Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 200 mg
Meclofenamic acidCat No HY-117275
Meclofenamic Acid a non-steroidalanti-inflammatory agent is a highly selectivefat mass and obesity-associated (FTO) enzymeinhibitor Meclofenamic Acid competes with FTObinding for the m(6)A-containing nucleic acid
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Rotigaptide (ZP123) Cat No HY-106225
Rotigaptide (ZP123) is a novel and specificmodulator of Rotigaptideconnexin 43 (Cx43)prevents the uncoupling of Cx43-mediated gap
communication and normalizes cell-to-celljunctioncommunication during acute metabolic stress
Purity 9963Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg
TAT-Gap19Cat No HY-P1136B
TAT-Gap19 a Cx mimetic peptide is a specific inhibitorconnexin43 hemichannel (Cx43 HC)
TAT-Gap19 does not inhibits the corresponding Cx43GJCs TAT-Gap19 traverses the blood-brain barrierand alleviate liver fibrosis in mice
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tonabersat (SB-220453) Cat No HY-15204
Tonabersat (SB-220453) is a modulatorgap-junctionTonabersat prevents inflammatory damage in thecentral nervous system
Purity 9968Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
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Integrin
Integrins a family of heterodimeric adhesion receptors for diverse extracellular matrices have consistently been implicated ascrucial drivers of ovarian cancer development and progression A number of the RGD-based members of the integrin familyincluding α5β1 and αvβ3 or αvβ5 integrins are markedly elevated in aggressive ovarian tumors These adhesion receptors appearto promote cell adhesion survival motility and invasion during ovarian tumor growth or metastatic progression Importantly thefunctions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signalingincluding the PI3KAkt- and RasMAPK-dependent pathways
Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion Modulationof these molecules particularly αv integrin family has exhibited profound effects on fibrosis in multiple organ and disease stateBased on the several studies the integrins αvβ3 αvβ5 αvβ6 and αvβ8 have been known to modulate the fibrotic process viaactivation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis
Each integrin is typically formed by the non-covalent pairing of one α subunit of which 18 types are known to exist and one βsubunit of which 8 types are known to exist Together 24 distinct heterodimers have been identified to date The αv subunit canform heterodimers with the β1 β3 β5 β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11 andαv indicating that not all theoretically possible α and subunit pairs form Interestingly the activation of TGF-β appears to be acommon function of multiple αv integrins
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Integrin Inhibitors Agonists Antagonists amp Modulators
A-205804Cat No HY-100226
A-205804 is an orally bioavailable potent andselective lead inhibitor of andE-selectin
expression with an of 20 nM and 25ICAM-1 IC50
nM for E-selectin and ICAM-1 respectivelyA-205804 can be used in the research of chronicinflammatory diseases
Purity 9812Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Arg-Gly-Asp-Ser (RGDS peptide Fibronectin tetrapeptide) Cat No HY-12290
Arg-Gly-Asp-Ser is an integrin binding sequencethat inhibits functionintegrin receptordecreases systemic inflammation via inhibition ofcollagen-triggered activation of leukocytes andattenuates expression of inflammatory cytokinesiNOS and MMP-9
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Arg-Gly-Asp-Ser (TFA) (RGDS peptide (TFA) Fibronectin tetrapeptide (TFA)) Cat No HY-12290A
Arg-Gly-Asp-Ser (TFA) is an integrin bindingsequence that inhibits functionintegrin receptorArg-Gly-Asp-Ser (TFA) directly and specificallybind pro-caspase-8 pro-caspase-9 andpro-caspase-3 while it does not bindpro-caspase-1
Purity gt98Clinical DataSize 1 mg 5 mg
ATN-161 trifluoroacetate salt (ATN-161 TFA salt) Cat No HY-13535A
ATN-161 trifluoroacetate salt is a novel integrin antagonist which inhibits angiogenesis andα5β1
growth of liver metastases in a murine model
Purity ge950Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg
BI-1950Cat No HY-124040
BI-1950 is a highly potent lymphocyte function inhibitor LFA-1 isassociated antigen-1 (LFA-1)
an essential component in normal immune systemfunction and a target for drug discovery
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO-1211Cat No HY-14126
BIO-1211 is a highly selective and orally active inhibitor with values of 4 nMα4β1 (VLA-4) IC50
and 2 μM for α4β1 and α4β7 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192Cat No HY-107589
BIO5192 is a selective and potent integrin α4β1(VLA-4) inhibitor ( lt10 pM) BIO5192Kd
selectively binds to α4β1 ( =18 nM) over aIC50
range of other integrins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192 hydrateCat No HY-107589A
BIO5192 hydrate is a selective and potent integrin inhibitor ( lt10 pM) BIO5192α4β1 (VLA-4) Kd
hydrate selectively binds to α4β1 ( =18 nM)IC50
over a range of other integrins
Purity ge980Clinical Data No Development ReportedSize 1 mg
BMS-688521Cat No HY-10596
BMS-688521 is a highly potent orally activeinhibitor of the interaction withLFA-1ICAMan of 25 nM in the adhesion assay and anIC50
of 60 nM in the MLR assay BMS-688521 isIC50
efficacious in a mouse allergic eosinophilic lunginflammation model
Purity 9925Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
BOP sodiumCat No HY-129453
BOP sodium is a potent and selective dual inhibitor with values inα9β1α4β1 integrin Kd
the picomolar range BOP sodium shows the rapidand preferential mobilization of hematopoieticstem cell (HSC) and progenitors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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c(phg-isoDGR-(NMe)k)Cat No HY-111413
c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
c(phg-isoDGR-(NMe)k) TFACat No HY-111413A
c(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
CarotegrastCat No HY-14857
Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor
activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Carotegrast methyl (AJM300) Cat No HY-124290
Carotegrast methyl (AJM300) is an orally activeand selective antagonist HCA2969 anα4 integrinactive metabolite of AJM300 is a specific dualα4β1α4β7 integrin antagonist Carotegrast methylprevents the development of colitis in miceltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cilengitide (EMD 121974) Cat No HY-16141
Cilengitide (EMD 121974) is a potent and selectiveinhibitor of the and integrins α βν 3 α βν 5
Cilengitide inhibits binding of isolated α βν 3
and α β to Vitronectin with an IC value of 4ν 5 50
and 79 nM respectively
Purity 9932Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cilengitide TFA (EMD 121974 TFA) Cat No HY-16143
Cilengitide is a potent and selective integrininhibitor for α β and α β receptor withv 3 v 5
values of 4 nM and 79 nM respectivelyIC50
Purity 9885Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Cucurbitacin BCat No HY-N0416
Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids could represscancer cell progression
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
CWHM-12Cat No HY-18644
CWHM-12 is a potent inhibitor of withαV integrinss of 02 08 15 and 18 nM for IC50 αvβ8
and αvβ3 αvβ6 αvβ1
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK)Cat No HY-P0023
Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin with an of 094 nMα βv 3 IC50
Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK) TFACat No HY-P0023A
Cyclo(-RGDfK) TFA is a potent and selectiveinhibitor of the integrin with an ofα βv 3 IC50
094 nM Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity 9981Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
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Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat No HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof with antitumor activityintegrin αvβ3
Purity 9940Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RADfK)Cat No HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch therapy and diagnosis ofneoangiogenesis
Purity 9803Clinical Data No Development ReportedSize 1 mg
Cyclo(RGDyK)Cat No HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nMintegrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RGDyK) trifluoroacetateCat No HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
E7820 (ER68203-00) Cat No HY-14571
E7820 (ER68203-00) an orally active aromaticsulfonamide derivative is a unique angiogenesisinhibitor suppressing an expression of integrin
subunit on endothelium E7820 inhibits ratalpha2aorta angiogenesis with an of 011 μgmlIC50
Purity 9936Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
EchistatinCat No HY-P1189
Echistatin the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Echistatin TFACat No HY-P1189A
Echistatin TFA the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EptifibatideCat No HY-B0686
Eptifibatide is a cyclic heptapeptide acts as acompetitive antagonist for the activated platelet
with anti-plateletglycoprotein IIbIIIa receptoractivity
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Eptifibatide acetateCat No HY-B0686A
Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Firategrast (SB 683699) Cat No HY-14951
Firategrast (SB 683699) is an orally active andspecific antagonistα4β1α4β7 integrinFirategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) anddecreases multiple sclerosis (MS) activity
Purity 9988Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
wwwMedChemExpresscom 15
ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
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SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
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Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
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MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
24 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
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BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
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DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 35
Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
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Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 51
ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
Arp23 ComplexActin-related protein 23 complex
The intact ARP23 complex is first purified from based on its affinity for the actin-binding protein profilinAcanthamoeba castellaniiand is shown to consist of a stable assembly of seven polypeptides Two of the subunits are actin-related proteins of the ARP2 andARP3 subfamilies giving the complex its name
The ARP23 complex possesses little biochemical activity on its own However when engaged by nucleation-promoting factor (NPF)proteins it is activated to initiate the formation of a new (daughter) filament that emerges from an existing (mother) filament in ay-branch configuration with a regular 70deg branch angle This coupling of nucleation and branching by the ARP23 complex isreferred to as autocatalytic branching or dendritic nucleation and is central to its functions in vivo
Polymerization of actin filaments directed by the Arp23 complex supports many types of cellular movements
wwwMedChemExpresscom 3
Arp23 Complex Inhibitors amp Activators
187-1 N-WASP inhibitorCat No HY-P1045
187-1 N-WASP inhibitor a 14-aa cyclic peptideis an allosteric neural Wiskott-Aldrich syndrome
inhibitor 187-1 N-WASPprotein (N-WASP)inhibitor potently inhibits actin assembly inducedby phosphatidylinositol 45-bisphosphate (PIP2)with an of 2 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
187-1 N-WASP inhibitor TFACat No HY-P1045A
187-1 N-WASP inhibitor TFA a 14-aa cyclicpeptide is an allosteric neural Wiskott-Aldrich
inhibitorsyndrome protein (N-WASP)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Benproperine phosphateCat No HY-114657A
Benproperine phosphate is an orally active potentactin-related protein 23 complex subunit 2
inhibitor Benproperine phosphate(ARPC2)attenuates the actin polymerization rate of actionpolymerization nucleation by impairing Arp23function
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
CK-636 (CK-0944636) Cat No HY-15892
CK-636 is a cell permeable inhibitor of Arp23 that could inhibit actincomplex
polymerization with values of 4 μM 24 μMIC50
and 32 μM for human fission yeast and bovinerespectively
Purity 9843Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
CK-666Cat No HY-16926
CK-666 is a cell-permeable actin-related protein inhibitor ( =12 μM) CK-666Arp23 complex IC50
binds to Arp23 complex stabilizes the inactivestate of the complex blocking movement of theArp2 and Arp3 subunits into the activatedfilament-like (short pitch) conformation
Purity 9963Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
CK-869Cat No HY-16927
CK-869 is an Actin-Related Protein 23 (ARP23)complex inhibitor with an of 7 μMIC50
Purity 9976Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Cytochalasin B (Phomin) Cat No HY-16928
Cytochalasin B is a cell-permeable mycotoxinbinding to the barbed end of filamentsactindisrupting the formation of actin polymers with
value of 14-22 nM for F-actinKd
Purity 9892Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Cytochalasin D (Zygosporin A NSC 209835) Cat No HY-N6682
Cytochalasin D (Zygosporin A NSC 209835) is apotent and cell-permeable inhibitor of actinpolymerization derived from fungus inhibits theG-actinndashcofilin interaction by binding to G-actin
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
Dihydrocytochalasin BCat No HY-N6701
Dihydrocytochalasin B (H2CB) is a Cytokinesisinhibitor and changes the morphology of the cellssimilar to that of cytochalasin B does notinhibit glucose transport
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
JasplakinolideCat No HY-P0027
Jasplakinolide is a potent actin polymerizationinducer and stabilizes pre-existing actinfilaments Jasplakinolide binds to F-actincompetitively with phalloidin with a of 15Kd
nM
Purity ge980Clinical Data No Development ReportedSize 100 μg
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Latrunculin A (LAT-A) Cat No HY-16929
Latrunculin A (LAT-A) is a toxin isolated from thered sea sponge binds toLatrunculia magnificaactin monomers inhibits polymerization of actinwith s of 01 04 47 μM and 019 μM forKd
ATP-actin ADP-Pi-actin ADP-actin and G-actinrespectively
Purity ge980Clinical Data No Development ReportedSize 100 μg
wwwMedChemExpresscom 5
Dynamin
Dynamins are large superfamily GTPase proteins that are involved in various cellular processes including budding of transportvesicles division of organelles cytokinesis and pathogen resistance Dynamins are involved in scission (cleavage of the vesicle fromthe parent membrane) of nascent vesicles from parent membranes in eukaryotic cells Dynamins interact directly with the lipidbilayer at the necks of clathrin-coated pits to sever and release coated vesicles Dynamins contain five domains including GTPasedomain middle domain PH domain GTPase effector domain (GED) and proline rich domain (PRD) while the dynamin-relatedproteins (DRPs) lack one or more of these domains or have additional domains Dynamins and DRPs participate in a wide variety ofcellular processes including budding mitochondrial fission (mammalian Dlp1 and Dnm1) and fusionSaccharomyces cerevisiae(mammalian OPA1 Mgm1 and Msp1) vacuolar fission ( Vps1)Scerevisiae Schizosaccharomycespombe S cerevisiaeinterferon-induced anti-viral protection (fish Mx proteins) plant cell cytokinesis and membrane fission ( DRPArabidopsis thalianaproteins) as well as pathogen resistance
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Dynamin Inhibitors
Dynamin inhibitory peptideCat No HY-P1083
Dynamin inhibitory peptide competitively blocksbinding of to amphiphysin thusdynaminpreventing endocytosis Dynamin inhibitory peptideblocks the dopamine D3 effect on GABAA receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Dynamin inhibitory peptide TFACat No HY-P1083A
Dynamin inhibitory peptide TFA competitivelyblocks binding of to amphiphysin thusdynaminpreventing endocytosis Dynamin inhibitory peptideTFA blocks the dopamine D effect on GABA3 A
receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynaMin inhibitory peptide myristoylatedCat No HY-P1369
DynaMin inhibitory peptide myristoylated is a inhibitor to interfere with the bindingDynaMin
of amphiphysin with dynamin DynaMin inhibitorypeptide myristoylated is a membrane-permeant formof the peptide that prevents endocytosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynaMin inhibitory peptide myristoylated TFACat No HY-P1369A
DynaMin inhibitory peptide myristoylated TFA is a inhibitor to interfere with the bindingDynaMin
of amphiphysin with dynamin DynaMin inhibitorypeptide myristoylated TFA is a membrane-permeantform of the peptide that prevents endocytosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynasoreCat No HY-15304
Dynasore is a cell-permeable inhibitordynaminwith an of 15 μMIC50
Purity 9870Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Hydroxy-Dynasore (Dyngo-4a) Cat No HY-13863
Hydroxy Dynasore (Dyngo-4a) a structural analogof Dynasore (HY-15304) is an potency improvedlow cytotoxicity and nonspecific binding
inhibitor with values of 038dynamin IC50
μM and 23 μM for brain dynamin I andrecombinant rat dynamin II respectively
Purity 9614Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Mdivi-1 (Mitochondrial division inhibitor 1) Cat No HY-15886
Mdivi-1 is a selective dynamin-related protein 1( ) inhibitor Mdivi-1 is a mitochondrialDrp1division inhibitormitophagy
Purity 9973Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SchaftosideCat No HY-N0703
Schaftoside is a flavonoid found in a variety ofChinese herbal medicines such as Eleusine indicaSchaftoside inhibits the expression of TLR4 andMyd88 Schaftoside also decreases Drp1 expressionand phosphorylation and reduces mitochondrialfission
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 20 mg
wwwMedChemExpresscom 7
Gap Junction Protein
Gap junction channels are essential in normal heart function and they assist in the mediated spread of electrical impulses thatstimulate synchronized contraction (via an electrical syncytium) of cardiac tissues
Gap junction (GJ) proteins play an important role in direct communication between cells of many tissue types GJs are specialisedintercellular membrane-spanning domains that allow the passage of small molecules including second messenger (eg c-AMPinositol triphosphate) or ionic signals from one cell to another GJ proteins and their long evolutionary history have permittedadaptation of gap junction intercellular communication (GJIC) with several important functions and multiple regulatory processesFormation of GJIC is an essential mechanism in coordinating growth and development and tissue compartmentalization duringembryonic development
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Gap Junction Protein Inhibitors amp Modulators
AT-1002Cat No HY-114426
AT-1002 a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AT-1002 TFACat No HY-114426A
AT-1002 TFA a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Carbenoxolone disodiumCat No HY-B1367
Carbenoxolone disodium is the active metaboliteof Glycyrrhizic acid (HY-N0184) and the inhibitorof human and bacterial 11β-HSD 3α 20β-HSDCarbenoxolone disodium is an uncoupling agent for
and a potent inhibitor of gap junctions Vacciniavirus replication
Purity 9929Clinical Data LaunchedSize 10 mM times 1 mL 25 mg 50 mg 100 mg
Danegaptide (GAP-134 ZP 1609) Cat No HY-10913
Danegaptide (GAP-134) is a potent selective andorally active modifier with angap-junctionantiarrhythmic effect
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
Danegaptide Hydrochloride (GAP-134 Hydrochloride ZP 1609 Hydrochloride) Cat No HY-10913A
Danegaptide Hydrochloride (GAP-134 Hydrochloride)is a potent selective and orally active
modifier with an antiarrhythmicgap-junctioneffect
Purity 9975Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Gap 26Cat No HY-P1082
Gap 26 is a connexin mimetic peptide composed ofresidue numbers 63-75 of the first extracellularloop of connexin 43 (gap junction blocker)containing the SHVR amino acid motif
Purity 9964Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 26 TFACat No HY-P1082A
Gap 26 TFA is a connexin mimetic peptide composedof residue numbers 63-75 of the firstextracellular loop of connexin 43 (gap junctionblocker) containing the SHVR amino acid motif
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 27Cat No HY-P0139
Gap 27 a synthetic connexin43 mimetic peptide isa gap junction inhibitor Gap 27 possessesconserved sequence homology to a portion of thesecond extracellular loop leading into the fourthtransmembrane connexin segment
Purity 9807Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19Cat No HY-P1136
Gap19 a peptide derived from nine amino acids ofthe Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19 TFACat No HY-P1136A
Gap19 TFA a peptide derived from nine amino acidsof the Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 TFA inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
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Larazotide acetateCat No HY-106268A
Larazotide acetate is a synthetic peptideLarazotide acetate acts as a tight junctionregulator and reverses leaky junctions to theirnormally closed state
Purity 9968Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Meclofenamate sodium (Meclofenamic acid sodium) Cat No HY-B1320
Meclofenamic acid sodium is a nonsteroidalanti-inflammatory drug (NSAID) approved for use inarthritis (osteo and rheumatoid) analgesia (mildto moderate pain) dysmenorrhea and heavymenstrual blood loss (menorrhagia)
Purity 9862Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 200 mg
Meclofenamic acidCat No HY-117275
Meclofenamic Acid a non-steroidalanti-inflammatory agent is a highly selectivefat mass and obesity-associated (FTO) enzymeinhibitor Meclofenamic Acid competes with FTObinding for the m(6)A-containing nucleic acid
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Rotigaptide (ZP123) Cat No HY-106225
Rotigaptide (ZP123) is a novel and specificmodulator of Rotigaptideconnexin 43 (Cx43)prevents the uncoupling of Cx43-mediated gap
communication and normalizes cell-to-celljunctioncommunication during acute metabolic stress
Purity 9963Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg
TAT-Gap19Cat No HY-P1136B
TAT-Gap19 a Cx mimetic peptide is a specific inhibitorconnexin43 hemichannel (Cx43 HC)
TAT-Gap19 does not inhibits the corresponding Cx43GJCs TAT-Gap19 traverses the blood-brain barrierand alleviate liver fibrosis in mice
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tonabersat (SB-220453) Cat No HY-15204
Tonabersat (SB-220453) is a modulatorgap-junctionTonabersat prevents inflammatory damage in thecentral nervous system
Purity 9968Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
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Integrin
Integrins a family of heterodimeric adhesion receptors for diverse extracellular matrices have consistently been implicated ascrucial drivers of ovarian cancer development and progression A number of the RGD-based members of the integrin familyincluding α5β1 and αvβ3 or αvβ5 integrins are markedly elevated in aggressive ovarian tumors These adhesion receptors appearto promote cell adhesion survival motility and invasion during ovarian tumor growth or metastatic progression Importantly thefunctions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signalingincluding the PI3KAkt- and RasMAPK-dependent pathways
Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion Modulationof these molecules particularly αv integrin family has exhibited profound effects on fibrosis in multiple organ and disease stateBased on the several studies the integrins αvβ3 αvβ5 αvβ6 and αvβ8 have been known to modulate the fibrotic process viaactivation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis
Each integrin is typically formed by the non-covalent pairing of one α subunit of which 18 types are known to exist and one βsubunit of which 8 types are known to exist Together 24 distinct heterodimers have been identified to date The αv subunit canform heterodimers with the β1 β3 β5 β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11 andαv indicating that not all theoretically possible α and subunit pairs form Interestingly the activation of TGF-β appears to be acommon function of multiple αv integrins
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Integrin Inhibitors Agonists Antagonists amp Modulators
A-205804Cat No HY-100226
A-205804 is an orally bioavailable potent andselective lead inhibitor of andE-selectin
expression with an of 20 nM and 25ICAM-1 IC50
nM for E-selectin and ICAM-1 respectivelyA-205804 can be used in the research of chronicinflammatory diseases
Purity 9812Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Arg-Gly-Asp-Ser (RGDS peptide Fibronectin tetrapeptide) Cat No HY-12290
Arg-Gly-Asp-Ser is an integrin binding sequencethat inhibits functionintegrin receptordecreases systemic inflammation via inhibition ofcollagen-triggered activation of leukocytes andattenuates expression of inflammatory cytokinesiNOS and MMP-9
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Arg-Gly-Asp-Ser (TFA) (RGDS peptide (TFA) Fibronectin tetrapeptide (TFA)) Cat No HY-12290A
Arg-Gly-Asp-Ser (TFA) is an integrin bindingsequence that inhibits functionintegrin receptorArg-Gly-Asp-Ser (TFA) directly and specificallybind pro-caspase-8 pro-caspase-9 andpro-caspase-3 while it does not bindpro-caspase-1
Purity gt98Clinical DataSize 1 mg 5 mg
ATN-161 trifluoroacetate salt (ATN-161 TFA salt) Cat No HY-13535A
ATN-161 trifluoroacetate salt is a novel integrin antagonist which inhibits angiogenesis andα5β1
growth of liver metastases in a murine model
Purity ge950Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg
BI-1950Cat No HY-124040
BI-1950 is a highly potent lymphocyte function inhibitor LFA-1 isassociated antigen-1 (LFA-1)
an essential component in normal immune systemfunction and a target for drug discovery
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO-1211Cat No HY-14126
BIO-1211 is a highly selective and orally active inhibitor with values of 4 nMα4β1 (VLA-4) IC50
and 2 μM for α4β1 and α4β7 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192Cat No HY-107589
BIO5192 is a selective and potent integrin α4β1(VLA-4) inhibitor ( lt10 pM) BIO5192Kd
selectively binds to α4β1 ( =18 nM) over aIC50
range of other integrins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192 hydrateCat No HY-107589A
BIO5192 hydrate is a selective and potent integrin inhibitor ( lt10 pM) BIO5192α4β1 (VLA-4) Kd
hydrate selectively binds to α4β1 ( =18 nM)IC50
over a range of other integrins
Purity ge980Clinical Data No Development ReportedSize 1 mg
BMS-688521Cat No HY-10596
BMS-688521 is a highly potent orally activeinhibitor of the interaction withLFA-1ICAMan of 25 nM in the adhesion assay and anIC50
of 60 nM in the MLR assay BMS-688521 isIC50
efficacious in a mouse allergic eosinophilic lunginflammation model
Purity 9925Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
BOP sodiumCat No HY-129453
BOP sodium is a potent and selective dual inhibitor with values inα9β1α4β1 integrin Kd
the picomolar range BOP sodium shows the rapidand preferential mobilization of hematopoieticstem cell (HSC) and progenitors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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c(phg-isoDGR-(NMe)k)Cat No HY-111413
c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
c(phg-isoDGR-(NMe)k) TFACat No HY-111413A
c(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
CarotegrastCat No HY-14857
Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor
activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Carotegrast methyl (AJM300) Cat No HY-124290
Carotegrast methyl (AJM300) is an orally activeand selective antagonist HCA2969 anα4 integrinactive metabolite of AJM300 is a specific dualα4β1α4β7 integrin antagonist Carotegrast methylprevents the development of colitis in miceltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cilengitide (EMD 121974) Cat No HY-16141
Cilengitide (EMD 121974) is a potent and selectiveinhibitor of the and integrins α βν 3 α βν 5
Cilengitide inhibits binding of isolated α βν 3
and α β to Vitronectin with an IC value of 4ν 5 50
and 79 nM respectively
Purity 9932Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cilengitide TFA (EMD 121974 TFA) Cat No HY-16143
Cilengitide is a potent and selective integrininhibitor for α β and α β receptor withv 3 v 5
values of 4 nM and 79 nM respectivelyIC50
Purity 9885Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Cucurbitacin BCat No HY-N0416
Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids could represscancer cell progression
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
CWHM-12Cat No HY-18644
CWHM-12 is a potent inhibitor of withαV integrinss of 02 08 15 and 18 nM for IC50 αvβ8
and αvβ3 αvβ6 αvβ1
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK)Cat No HY-P0023
Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin with an of 094 nMα βv 3 IC50
Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK) TFACat No HY-P0023A
Cyclo(-RGDfK) TFA is a potent and selectiveinhibitor of the integrin with an ofα βv 3 IC50
094 nM Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity 9981Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
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Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat No HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof with antitumor activityintegrin αvβ3
Purity 9940Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RADfK)Cat No HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch therapy and diagnosis ofneoangiogenesis
Purity 9803Clinical Data No Development ReportedSize 1 mg
Cyclo(RGDyK)Cat No HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nMintegrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RGDyK) trifluoroacetateCat No HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
E7820 (ER68203-00) Cat No HY-14571
E7820 (ER68203-00) an orally active aromaticsulfonamide derivative is a unique angiogenesisinhibitor suppressing an expression of integrin
subunit on endothelium E7820 inhibits ratalpha2aorta angiogenesis with an of 011 μgmlIC50
Purity 9936Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
EchistatinCat No HY-P1189
Echistatin the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Echistatin TFACat No HY-P1189A
Echistatin TFA the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EptifibatideCat No HY-B0686
Eptifibatide is a cyclic heptapeptide acts as acompetitive antagonist for the activated platelet
with anti-plateletglycoprotein IIbIIIa receptoractivity
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Eptifibatide acetateCat No HY-B0686A
Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Firategrast (SB 683699) Cat No HY-14951
Firategrast (SB 683699) is an orally active andspecific antagonistα4β1α4β7 integrinFirategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) anddecreases multiple sclerosis (MS) activity
Purity 9988Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
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ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
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SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 19
Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 21
Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
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AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
wwwMedChemExpresscom 25
BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
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Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
wwwMedChemExpresscom 27
DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
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EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 35
Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
36 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
38 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 51
ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
Arp23 Complex Inhibitors amp Activators
187-1 N-WASP inhibitorCat No HY-P1045
187-1 N-WASP inhibitor a 14-aa cyclic peptideis an allosteric neural Wiskott-Aldrich syndrome
inhibitor 187-1 N-WASPprotein (N-WASP)inhibitor potently inhibits actin assembly inducedby phosphatidylinositol 45-bisphosphate (PIP2)with an of 2 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
187-1 N-WASP inhibitor TFACat No HY-P1045A
187-1 N-WASP inhibitor TFA a 14-aa cyclicpeptide is an allosteric neural Wiskott-Aldrich
inhibitorsyndrome protein (N-WASP)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Benproperine phosphateCat No HY-114657A
Benproperine phosphate is an orally active potentactin-related protein 23 complex subunit 2
inhibitor Benproperine phosphate(ARPC2)attenuates the actin polymerization rate of actionpolymerization nucleation by impairing Arp23function
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
CK-636 (CK-0944636) Cat No HY-15892
CK-636 is a cell permeable inhibitor of Arp23 that could inhibit actincomplex
polymerization with values of 4 μM 24 μMIC50
and 32 μM for human fission yeast and bovinerespectively
Purity 9843Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
CK-666Cat No HY-16926
CK-666 is a cell-permeable actin-related protein inhibitor ( =12 μM) CK-666Arp23 complex IC50
binds to Arp23 complex stabilizes the inactivestate of the complex blocking movement of theArp2 and Arp3 subunits into the activatedfilament-like (short pitch) conformation
Purity 9963Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
CK-869Cat No HY-16927
CK-869 is an Actin-Related Protein 23 (ARP23)complex inhibitor with an of 7 μMIC50
Purity 9976Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Cytochalasin B (Phomin) Cat No HY-16928
Cytochalasin B is a cell-permeable mycotoxinbinding to the barbed end of filamentsactindisrupting the formation of actin polymers with
value of 14-22 nM for F-actinKd
Purity 9892Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Cytochalasin D (Zygosporin A NSC 209835) Cat No HY-N6682
Cytochalasin D (Zygosporin A NSC 209835) is apotent and cell-permeable inhibitor of actinpolymerization derived from fungus inhibits theG-actinndashcofilin interaction by binding to G-actin
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
Dihydrocytochalasin BCat No HY-N6701
Dihydrocytochalasin B (H2CB) is a Cytokinesisinhibitor and changes the morphology of the cellssimilar to that of cytochalasin B does notinhibit glucose transport
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
JasplakinolideCat No HY-P0027
Jasplakinolide is a potent actin polymerizationinducer and stabilizes pre-existing actinfilaments Jasplakinolide binds to F-actincompetitively with phalloidin with a of 15Kd
nM
Purity ge980Clinical Data No Development ReportedSize 100 μg
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Latrunculin A (LAT-A) Cat No HY-16929
Latrunculin A (LAT-A) is a toxin isolated from thered sea sponge binds toLatrunculia magnificaactin monomers inhibits polymerization of actinwith s of 01 04 47 μM and 019 μM forKd
ATP-actin ADP-Pi-actin ADP-actin and G-actinrespectively
Purity ge980Clinical Data No Development ReportedSize 100 μg
wwwMedChemExpresscom 5
Dynamin
Dynamins are large superfamily GTPase proteins that are involved in various cellular processes including budding of transportvesicles division of organelles cytokinesis and pathogen resistance Dynamins are involved in scission (cleavage of the vesicle fromthe parent membrane) of nascent vesicles from parent membranes in eukaryotic cells Dynamins interact directly with the lipidbilayer at the necks of clathrin-coated pits to sever and release coated vesicles Dynamins contain five domains including GTPasedomain middle domain PH domain GTPase effector domain (GED) and proline rich domain (PRD) while the dynamin-relatedproteins (DRPs) lack one or more of these domains or have additional domains Dynamins and DRPs participate in a wide variety ofcellular processes including budding mitochondrial fission (mammalian Dlp1 and Dnm1) and fusionSaccharomyces cerevisiae(mammalian OPA1 Mgm1 and Msp1) vacuolar fission ( Vps1)Scerevisiae Schizosaccharomycespombe S cerevisiaeinterferon-induced anti-viral protection (fish Mx proteins) plant cell cytokinesis and membrane fission ( DRPArabidopsis thalianaproteins) as well as pathogen resistance
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Dynamin Inhibitors
Dynamin inhibitory peptideCat No HY-P1083
Dynamin inhibitory peptide competitively blocksbinding of to amphiphysin thusdynaminpreventing endocytosis Dynamin inhibitory peptideblocks the dopamine D3 effect on GABAA receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Dynamin inhibitory peptide TFACat No HY-P1083A
Dynamin inhibitory peptide TFA competitivelyblocks binding of to amphiphysin thusdynaminpreventing endocytosis Dynamin inhibitory peptideTFA blocks the dopamine D effect on GABA3 A
receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynaMin inhibitory peptide myristoylatedCat No HY-P1369
DynaMin inhibitory peptide myristoylated is a inhibitor to interfere with the bindingDynaMin
of amphiphysin with dynamin DynaMin inhibitorypeptide myristoylated is a membrane-permeant formof the peptide that prevents endocytosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynaMin inhibitory peptide myristoylated TFACat No HY-P1369A
DynaMin inhibitory peptide myristoylated TFA is a inhibitor to interfere with the bindingDynaMin
of amphiphysin with dynamin DynaMin inhibitorypeptide myristoylated TFA is a membrane-permeantform of the peptide that prevents endocytosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynasoreCat No HY-15304
Dynasore is a cell-permeable inhibitordynaminwith an of 15 μMIC50
Purity 9870Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Hydroxy-Dynasore (Dyngo-4a) Cat No HY-13863
Hydroxy Dynasore (Dyngo-4a) a structural analogof Dynasore (HY-15304) is an potency improvedlow cytotoxicity and nonspecific binding
inhibitor with values of 038dynamin IC50
μM and 23 μM for brain dynamin I andrecombinant rat dynamin II respectively
Purity 9614Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Mdivi-1 (Mitochondrial division inhibitor 1) Cat No HY-15886
Mdivi-1 is a selective dynamin-related protein 1( ) inhibitor Mdivi-1 is a mitochondrialDrp1division inhibitormitophagy
Purity 9973Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SchaftosideCat No HY-N0703
Schaftoside is a flavonoid found in a variety ofChinese herbal medicines such as Eleusine indicaSchaftoside inhibits the expression of TLR4 andMyd88 Schaftoside also decreases Drp1 expressionand phosphorylation and reduces mitochondrialfission
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 20 mg
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Gap Junction Protein
Gap junction channels are essential in normal heart function and they assist in the mediated spread of electrical impulses thatstimulate synchronized contraction (via an electrical syncytium) of cardiac tissues
Gap junction (GJ) proteins play an important role in direct communication between cells of many tissue types GJs are specialisedintercellular membrane-spanning domains that allow the passage of small molecules including second messenger (eg c-AMPinositol triphosphate) or ionic signals from one cell to another GJ proteins and their long evolutionary history have permittedadaptation of gap junction intercellular communication (GJIC) with several important functions and multiple regulatory processesFormation of GJIC is an essential mechanism in coordinating growth and development and tissue compartmentalization duringembryonic development
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Gap Junction Protein Inhibitors amp Modulators
AT-1002Cat No HY-114426
AT-1002 a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AT-1002 TFACat No HY-114426A
AT-1002 TFA a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Carbenoxolone disodiumCat No HY-B1367
Carbenoxolone disodium is the active metaboliteof Glycyrrhizic acid (HY-N0184) and the inhibitorof human and bacterial 11β-HSD 3α 20β-HSDCarbenoxolone disodium is an uncoupling agent for
and a potent inhibitor of gap junctions Vacciniavirus replication
Purity 9929Clinical Data LaunchedSize 10 mM times 1 mL 25 mg 50 mg 100 mg
Danegaptide (GAP-134 ZP 1609) Cat No HY-10913
Danegaptide (GAP-134) is a potent selective andorally active modifier with angap-junctionantiarrhythmic effect
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
Danegaptide Hydrochloride (GAP-134 Hydrochloride ZP 1609 Hydrochloride) Cat No HY-10913A
Danegaptide Hydrochloride (GAP-134 Hydrochloride)is a potent selective and orally active
modifier with an antiarrhythmicgap-junctioneffect
Purity 9975Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Gap 26Cat No HY-P1082
Gap 26 is a connexin mimetic peptide composed ofresidue numbers 63-75 of the first extracellularloop of connexin 43 (gap junction blocker)containing the SHVR amino acid motif
Purity 9964Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 26 TFACat No HY-P1082A
Gap 26 TFA is a connexin mimetic peptide composedof residue numbers 63-75 of the firstextracellular loop of connexin 43 (gap junctionblocker) containing the SHVR amino acid motif
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 27Cat No HY-P0139
Gap 27 a synthetic connexin43 mimetic peptide isa gap junction inhibitor Gap 27 possessesconserved sequence homology to a portion of thesecond extracellular loop leading into the fourthtransmembrane connexin segment
Purity 9807Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19Cat No HY-P1136
Gap19 a peptide derived from nine amino acids ofthe Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19 TFACat No HY-P1136A
Gap19 TFA a peptide derived from nine amino acidsof the Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 TFA inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
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Larazotide acetateCat No HY-106268A
Larazotide acetate is a synthetic peptideLarazotide acetate acts as a tight junctionregulator and reverses leaky junctions to theirnormally closed state
Purity 9968Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Meclofenamate sodium (Meclofenamic acid sodium) Cat No HY-B1320
Meclofenamic acid sodium is a nonsteroidalanti-inflammatory drug (NSAID) approved for use inarthritis (osteo and rheumatoid) analgesia (mildto moderate pain) dysmenorrhea and heavymenstrual blood loss (menorrhagia)
Purity 9862Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 200 mg
Meclofenamic acidCat No HY-117275
Meclofenamic Acid a non-steroidalanti-inflammatory agent is a highly selectivefat mass and obesity-associated (FTO) enzymeinhibitor Meclofenamic Acid competes with FTObinding for the m(6)A-containing nucleic acid
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Rotigaptide (ZP123) Cat No HY-106225
Rotigaptide (ZP123) is a novel and specificmodulator of Rotigaptideconnexin 43 (Cx43)prevents the uncoupling of Cx43-mediated gap
communication and normalizes cell-to-celljunctioncommunication during acute metabolic stress
Purity 9963Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg
TAT-Gap19Cat No HY-P1136B
TAT-Gap19 a Cx mimetic peptide is a specific inhibitorconnexin43 hemichannel (Cx43 HC)
TAT-Gap19 does not inhibits the corresponding Cx43GJCs TAT-Gap19 traverses the blood-brain barrierand alleviate liver fibrosis in mice
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tonabersat (SB-220453) Cat No HY-15204
Tonabersat (SB-220453) is a modulatorgap-junctionTonabersat prevents inflammatory damage in thecentral nervous system
Purity 9968Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
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Integrin
Integrins a family of heterodimeric adhesion receptors for diverse extracellular matrices have consistently been implicated ascrucial drivers of ovarian cancer development and progression A number of the RGD-based members of the integrin familyincluding α5β1 and αvβ3 or αvβ5 integrins are markedly elevated in aggressive ovarian tumors These adhesion receptors appearto promote cell adhesion survival motility and invasion during ovarian tumor growth or metastatic progression Importantly thefunctions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signalingincluding the PI3KAkt- and RasMAPK-dependent pathways
Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion Modulationof these molecules particularly αv integrin family has exhibited profound effects on fibrosis in multiple organ and disease stateBased on the several studies the integrins αvβ3 αvβ5 αvβ6 and αvβ8 have been known to modulate the fibrotic process viaactivation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis
Each integrin is typically formed by the non-covalent pairing of one α subunit of which 18 types are known to exist and one βsubunit of which 8 types are known to exist Together 24 distinct heterodimers have been identified to date The αv subunit canform heterodimers with the β1 β3 β5 β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11 andαv indicating that not all theoretically possible α and subunit pairs form Interestingly the activation of TGF-β appears to be acommon function of multiple αv integrins
wwwMedChemExpresscom 11
Integrin Inhibitors Agonists Antagonists amp Modulators
A-205804Cat No HY-100226
A-205804 is an orally bioavailable potent andselective lead inhibitor of andE-selectin
expression with an of 20 nM and 25ICAM-1 IC50
nM for E-selectin and ICAM-1 respectivelyA-205804 can be used in the research of chronicinflammatory diseases
Purity 9812Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Arg-Gly-Asp-Ser (RGDS peptide Fibronectin tetrapeptide) Cat No HY-12290
Arg-Gly-Asp-Ser is an integrin binding sequencethat inhibits functionintegrin receptordecreases systemic inflammation via inhibition ofcollagen-triggered activation of leukocytes andattenuates expression of inflammatory cytokinesiNOS and MMP-9
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Arg-Gly-Asp-Ser (TFA) (RGDS peptide (TFA) Fibronectin tetrapeptide (TFA)) Cat No HY-12290A
Arg-Gly-Asp-Ser (TFA) is an integrin bindingsequence that inhibits functionintegrin receptorArg-Gly-Asp-Ser (TFA) directly and specificallybind pro-caspase-8 pro-caspase-9 andpro-caspase-3 while it does not bindpro-caspase-1
Purity gt98Clinical DataSize 1 mg 5 mg
ATN-161 trifluoroacetate salt (ATN-161 TFA salt) Cat No HY-13535A
ATN-161 trifluoroacetate salt is a novel integrin antagonist which inhibits angiogenesis andα5β1
growth of liver metastases in a murine model
Purity ge950Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg
BI-1950Cat No HY-124040
BI-1950 is a highly potent lymphocyte function inhibitor LFA-1 isassociated antigen-1 (LFA-1)
an essential component in normal immune systemfunction and a target for drug discovery
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO-1211Cat No HY-14126
BIO-1211 is a highly selective and orally active inhibitor with values of 4 nMα4β1 (VLA-4) IC50
and 2 μM for α4β1 and α4β7 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192Cat No HY-107589
BIO5192 is a selective and potent integrin α4β1(VLA-4) inhibitor ( lt10 pM) BIO5192Kd
selectively binds to α4β1 ( =18 nM) over aIC50
range of other integrins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192 hydrateCat No HY-107589A
BIO5192 hydrate is a selective and potent integrin inhibitor ( lt10 pM) BIO5192α4β1 (VLA-4) Kd
hydrate selectively binds to α4β1 ( =18 nM)IC50
over a range of other integrins
Purity ge980Clinical Data No Development ReportedSize 1 mg
BMS-688521Cat No HY-10596
BMS-688521 is a highly potent orally activeinhibitor of the interaction withLFA-1ICAMan of 25 nM in the adhesion assay and anIC50
of 60 nM in the MLR assay BMS-688521 isIC50
efficacious in a mouse allergic eosinophilic lunginflammation model
Purity 9925Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
BOP sodiumCat No HY-129453
BOP sodium is a potent and selective dual inhibitor with values inα9β1α4β1 integrin Kd
the picomolar range BOP sodium shows the rapidand preferential mobilization of hematopoieticstem cell (HSC) and progenitors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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c(phg-isoDGR-(NMe)k)Cat No HY-111413
c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
c(phg-isoDGR-(NMe)k) TFACat No HY-111413A
c(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
CarotegrastCat No HY-14857
Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor
activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Carotegrast methyl (AJM300) Cat No HY-124290
Carotegrast methyl (AJM300) is an orally activeand selective antagonist HCA2969 anα4 integrinactive metabolite of AJM300 is a specific dualα4β1α4β7 integrin antagonist Carotegrast methylprevents the development of colitis in miceltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cilengitide (EMD 121974) Cat No HY-16141
Cilengitide (EMD 121974) is a potent and selectiveinhibitor of the and integrins α βν 3 α βν 5
Cilengitide inhibits binding of isolated α βν 3
and α β to Vitronectin with an IC value of 4ν 5 50
and 79 nM respectively
Purity 9932Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cilengitide TFA (EMD 121974 TFA) Cat No HY-16143
Cilengitide is a potent and selective integrininhibitor for α β and α β receptor withv 3 v 5
values of 4 nM and 79 nM respectivelyIC50
Purity 9885Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Cucurbitacin BCat No HY-N0416
Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids could represscancer cell progression
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
CWHM-12Cat No HY-18644
CWHM-12 is a potent inhibitor of withαV integrinss of 02 08 15 and 18 nM for IC50 αvβ8
and αvβ3 αvβ6 αvβ1
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK)Cat No HY-P0023
Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin with an of 094 nMα βv 3 IC50
Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK) TFACat No HY-P0023A
Cyclo(-RGDfK) TFA is a potent and selectiveinhibitor of the integrin with an ofα βv 3 IC50
094 nM Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity 9981Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
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Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat No HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof with antitumor activityintegrin αvβ3
Purity 9940Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RADfK)Cat No HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch therapy and diagnosis ofneoangiogenesis
Purity 9803Clinical Data No Development ReportedSize 1 mg
Cyclo(RGDyK)Cat No HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nMintegrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RGDyK) trifluoroacetateCat No HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
E7820 (ER68203-00) Cat No HY-14571
E7820 (ER68203-00) an orally active aromaticsulfonamide derivative is a unique angiogenesisinhibitor suppressing an expression of integrin
subunit on endothelium E7820 inhibits ratalpha2aorta angiogenesis with an of 011 μgmlIC50
Purity 9936Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
EchistatinCat No HY-P1189
Echistatin the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Echistatin TFACat No HY-P1189A
Echistatin TFA the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EptifibatideCat No HY-B0686
Eptifibatide is a cyclic heptapeptide acts as acompetitive antagonist for the activated platelet
with anti-plateletglycoprotein IIbIIIa receptoractivity
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Eptifibatide acetateCat No HY-B0686A
Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Firategrast (SB 683699) Cat No HY-14951
Firategrast (SB 683699) is an orally active andspecific antagonistα4β1α4β7 integrinFirategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) anddecreases multiple sclerosis (MS) activity
Purity 9988Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
wwwMedChemExpresscom 15
ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
wwwMedChemExpresscom 17
SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 19
Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 21
Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
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AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
wwwMedChemExpresscom 25
BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
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Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
wwwMedChemExpresscom 27
DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 35
Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
36 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
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ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
Latrunculin A (LAT-A) Cat No HY-16929
Latrunculin A (LAT-A) is a toxin isolated from thered sea sponge binds toLatrunculia magnificaactin monomers inhibits polymerization of actinwith s of 01 04 47 μM and 019 μM forKd
ATP-actin ADP-Pi-actin ADP-actin and G-actinrespectively
Purity ge980Clinical Data No Development ReportedSize 100 μg
wwwMedChemExpresscom 5
Dynamin
Dynamins are large superfamily GTPase proteins that are involved in various cellular processes including budding of transportvesicles division of organelles cytokinesis and pathogen resistance Dynamins are involved in scission (cleavage of the vesicle fromthe parent membrane) of nascent vesicles from parent membranes in eukaryotic cells Dynamins interact directly with the lipidbilayer at the necks of clathrin-coated pits to sever and release coated vesicles Dynamins contain five domains including GTPasedomain middle domain PH domain GTPase effector domain (GED) and proline rich domain (PRD) while the dynamin-relatedproteins (DRPs) lack one or more of these domains or have additional domains Dynamins and DRPs participate in a wide variety ofcellular processes including budding mitochondrial fission (mammalian Dlp1 and Dnm1) and fusionSaccharomyces cerevisiae(mammalian OPA1 Mgm1 and Msp1) vacuolar fission ( Vps1)Scerevisiae Schizosaccharomycespombe S cerevisiaeinterferon-induced anti-viral protection (fish Mx proteins) plant cell cytokinesis and membrane fission ( DRPArabidopsis thalianaproteins) as well as pathogen resistance
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Dynamin Inhibitors
Dynamin inhibitory peptideCat No HY-P1083
Dynamin inhibitory peptide competitively blocksbinding of to amphiphysin thusdynaminpreventing endocytosis Dynamin inhibitory peptideblocks the dopamine D3 effect on GABAA receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Dynamin inhibitory peptide TFACat No HY-P1083A
Dynamin inhibitory peptide TFA competitivelyblocks binding of to amphiphysin thusdynaminpreventing endocytosis Dynamin inhibitory peptideTFA blocks the dopamine D effect on GABA3 A
receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynaMin inhibitory peptide myristoylatedCat No HY-P1369
DynaMin inhibitory peptide myristoylated is a inhibitor to interfere with the bindingDynaMin
of amphiphysin with dynamin DynaMin inhibitorypeptide myristoylated is a membrane-permeant formof the peptide that prevents endocytosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynaMin inhibitory peptide myristoylated TFACat No HY-P1369A
DynaMin inhibitory peptide myristoylated TFA is a inhibitor to interfere with the bindingDynaMin
of amphiphysin with dynamin DynaMin inhibitorypeptide myristoylated TFA is a membrane-permeantform of the peptide that prevents endocytosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynasoreCat No HY-15304
Dynasore is a cell-permeable inhibitordynaminwith an of 15 μMIC50
Purity 9870Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Hydroxy-Dynasore (Dyngo-4a) Cat No HY-13863
Hydroxy Dynasore (Dyngo-4a) a structural analogof Dynasore (HY-15304) is an potency improvedlow cytotoxicity and nonspecific binding
inhibitor with values of 038dynamin IC50
μM and 23 μM for brain dynamin I andrecombinant rat dynamin II respectively
Purity 9614Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Mdivi-1 (Mitochondrial division inhibitor 1) Cat No HY-15886
Mdivi-1 is a selective dynamin-related protein 1( ) inhibitor Mdivi-1 is a mitochondrialDrp1division inhibitormitophagy
Purity 9973Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SchaftosideCat No HY-N0703
Schaftoside is a flavonoid found in a variety ofChinese herbal medicines such as Eleusine indicaSchaftoside inhibits the expression of TLR4 andMyd88 Schaftoside also decreases Drp1 expressionand phosphorylation and reduces mitochondrialfission
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 20 mg
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Gap Junction Protein
Gap junction channels are essential in normal heart function and they assist in the mediated spread of electrical impulses thatstimulate synchronized contraction (via an electrical syncytium) of cardiac tissues
Gap junction (GJ) proteins play an important role in direct communication between cells of many tissue types GJs are specialisedintercellular membrane-spanning domains that allow the passage of small molecules including second messenger (eg c-AMPinositol triphosphate) or ionic signals from one cell to another GJ proteins and their long evolutionary history have permittedadaptation of gap junction intercellular communication (GJIC) with several important functions and multiple regulatory processesFormation of GJIC is an essential mechanism in coordinating growth and development and tissue compartmentalization duringembryonic development
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Gap Junction Protein Inhibitors amp Modulators
AT-1002Cat No HY-114426
AT-1002 a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AT-1002 TFACat No HY-114426A
AT-1002 TFA a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Carbenoxolone disodiumCat No HY-B1367
Carbenoxolone disodium is the active metaboliteof Glycyrrhizic acid (HY-N0184) and the inhibitorof human and bacterial 11β-HSD 3α 20β-HSDCarbenoxolone disodium is an uncoupling agent for
and a potent inhibitor of gap junctions Vacciniavirus replication
Purity 9929Clinical Data LaunchedSize 10 mM times 1 mL 25 mg 50 mg 100 mg
Danegaptide (GAP-134 ZP 1609) Cat No HY-10913
Danegaptide (GAP-134) is a potent selective andorally active modifier with angap-junctionantiarrhythmic effect
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
Danegaptide Hydrochloride (GAP-134 Hydrochloride ZP 1609 Hydrochloride) Cat No HY-10913A
Danegaptide Hydrochloride (GAP-134 Hydrochloride)is a potent selective and orally active
modifier with an antiarrhythmicgap-junctioneffect
Purity 9975Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Gap 26Cat No HY-P1082
Gap 26 is a connexin mimetic peptide composed ofresidue numbers 63-75 of the first extracellularloop of connexin 43 (gap junction blocker)containing the SHVR amino acid motif
Purity 9964Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 26 TFACat No HY-P1082A
Gap 26 TFA is a connexin mimetic peptide composedof residue numbers 63-75 of the firstextracellular loop of connexin 43 (gap junctionblocker) containing the SHVR amino acid motif
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 27Cat No HY-P0139
Gap 27 a synthetic connexin43 mimetic peptide isa gap junction inhibitor Gap 27 possessesconserved sequence homology to a portion of thesecond extracellular loop leading into the fourthtransmembrane connexin segment
Purity 9807Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19Cat No HY-P1136
Gap19 a peptide derived from nine amino acids ofthe Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19 TFACat No HY-P1136A
Gap19 TFA a peptide derived from nine amino acidsof the Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 TFA inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
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Larazotide acetateCat No HY-106268A
Larazotide acetate is a synthetic peptideLarazotide acetate acts as a tight junctionregulator and reverses leaky junctions to theirnormally closed state
Purity 9968Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Meclofenamate sodium (Meclofenamic acid sodium) Cat No HY-B1320
Meclofenamic acid sodium is a nonsteroidalanti-inflammatory drug (NSAID) approved for use inarthritis (osteo and rheumatoid) analgesia (mildto moderate pain) dysmenorrhea and heavymenstrual blood loss (menorrhagia)
Purity 9862Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 200 mg
Meclofenamic acidCat No HY-117275
Meclofenamic Acid a non-steroidalanti-inflammatory agent is a highly selectivefat mass and obesity-associated (FTO) enzymeinhibitor Meclofenamic Acid competes with FTObinding for the m(6)A-containing nucleic acid
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Rotigaptide (ZP123) Cat No HY-106225
Rotigaptide (ZP123) is a novel and specificmodulator of Rotigaptideconnexin 43 (Cx43)prevents the uncoupling of Cx43-mediated gap
communication and normalizes cell-to-celljunctioncommunication during acute metabolic stress
Purity 9963Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg
TAT-Gap19Cat No HY-P1136B
TAT-Gap19 a Cx mimetic peptide is a specific inhibitorconnexin43 hemichannel (Cx43 HC)
TAT-Gap19 does not inhibits the corresponding Cx43GJCs TAT-Gap19 traverses the blood-brain barrierand alleviate liver fibrosis in mice
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tonabersat (SB-220453) Cat No HY-15204
Tonabersat (SB-220453) is a modulatorgap-junctionTonabersat prevents inflammatory damage in thecentral nervous system
Purity 9968Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
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Integrin
Integrins a family of heterodimeric adhesion receptors for diverse extracellular matrices have consistently been implicated ascrucial drivers of ovarian cancer development and progression A number of the RGD-based members of the integrin familyincluding α5β1 and αvβ3 or αvβ5 integrins are markedly elevated in aggressive ovarian tumors These adhesion receptors appearto promote cell adhesion survival motility and invasion during ovarian tumor growth or metastatic progression Importantly thefunctions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signalingincluding the PI3KAkt- and RasMAPK-dependent pathways
Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion Modulationof these molecules particularly αv integrin family has exhibited profound effects on fibrosis in multiple organ and disease stateBased on the several studies the integrins αvβ3 αvβ5 αvβ6 and αvβ8 have been known to modulate the fibrotic process viaactivation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis
Each integrin is typically formed by the non-covalent pairing of one α subunit of which 18 types are known to exist and one βsubunit of which 8 types are known to exist Together 24 distinct heterodimers have been identified to date The αv subunit canform heterodimers with the β1 β3 β5 β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11 andαv indicating that not all theoretically possible α and subunit pairs form Interestingly the activation of TGF-β appears to be acommon function of multiple αv integrins
wwwMedChemExpresscom 11
Integrin Inhibitors Agonists Antagonists amp Modulators
A-205804Cat No HY-100226
A-205804 is an orally bioavailable potent andselective lead inhibitor of andE-selectin
expression with an of 20 nM and 25ICAM-1 IC50
nM for E-selectin and ICAM-1 respectivelyA-205804 can be used in the research of chronicinflammatory diseases
Purity 9812Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Arg-Gly-Asp-Ser (RGDS peptide Fibronectin tetrapeptide) Cat No HY-12290
Arg-Gly-Asp-Ser is an integrin binding sequencethat inhibits functionintegrin receptordecreases systemic inflammation via inhibition ofcollagen-triggered activation of leukocytes andattenuates expression of inflammatory cytokinesiNOS and MMP-9
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Arg-Gly-Asp-Ser (TFA) (RGDS peptide (TFA) Fibronectin tetrapeptide (TFA)) Cat No HY-12290A
Arg-Gly-Asp-Ser (TFA) is an integrin bindingsequence that inhibits functionintegrin receptorArg-Gly-Asp-Ser (TFA) directly and specificallybind pro-caspase-8 pro-caspase-9 andpro-caspase-3 while it does not bindpro-caspase-1
Purity gt98Clinical DataSize 1 mg 5 mg
ATN-161 trifluoroacetate salt (ATN-161 TFA salt) Cat No HY-13535A
ATN-161 trifluoroacetate salt is a novel integrin antagonist which inhibits angiogenesis andα5β1
growth of liver metastases in a murine model
Purity ge950Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg
BI-1950Cat No HY-124040
BI-1950 is a highly potent lymphocyte function inhibitor LFA-1 isassociated antigen-1 (LFA-1)
an essential component in normal immune systemfunction and a target for drug discovery
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO-1211Cat No HY-14126
BIO-1211 is a highly selective and orally active inhibitor with values of 4 nMα4β1 (VLA-4) IC50
and 2 μM for α4β1 and α4β7 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192Cat No HY-107589
BIO5192 is a selective and potent integrin α4β1(VLA-4) inhibitor ( lt10 pM) BIO5192Kd
selectively binds to α4β1 ( =18 nM) over aIC50
range of other integrins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192 hydrateCat No HY-107589A
BIO5192 hydrate is a selective and potent integrin inhibitor ( lt10 pM) BIO5192α4β1 (VLA-4) Kd
hydrate selectively binds to α4β1 ( =18 nM)IC50
over a range of other integrins
Purity ge980Clinical Data No Development ReportedSize 1 mg
BMS-688521Cat No HY-10596
BMS-688521 is a highly potent orally activeinhibitor of the interaction withLFA-1ICAMan of 25 nM in the adhesion assay and anIC50
of 60 nM in the MLR assay BMS-688521 isIC50
efficacious in a mouse allergic eosinophilic lunginflammation model
Purity 9925Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
BOP sodiumCat No HY-129453
BOP sodium is a potent and selective dual inhibitor with values inα9β1α4β1 integrin Kd
the picomolar range BOP sodium shows the rapidand preferential mobilization of hematopoieticstem cell (HSC) and progenitors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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c(phg-isoDGR-(NMe)k)Cat No HY-111413
c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
c(phg-isoDGR-(NMe)k) TFACat No HY-111413A
c(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
CarotegrastCat No HY-14857
Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor
activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Carotegrast methyl (AJM300) Cat No HY-124290
Carotegrast methyl (AJM300) is an orally activeand selective antagonist HCA2969 anα4 integrinactive metabolite of AJM300 is a specific dualα4β1α4β7 integrin antagonist Carotegrast methylprevents the development of colitis in miceltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cilengitide (EMD 121974) Cat No HY-16141
Cilengitide (EMD 121974) is a potent and selectiveinhibitor of the and integrins α βν 3 α βν 5
Cilengitide inhibits binding of isolated α βν 3
and α β to Vitronectin with an IC value of 4ν 5 50
and 79 nM respectively
Purity 9932Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cilengitide TFA (EMD 121974 TFA) Cat No HY-16143
Cilengitide is a potent and selective integrininhibitor for α β and α β receptor withv 3 v 5
values of 4 nM and 79 nM respectivelyIC50
Purity 9885Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Cucurbitacin BCat No HY-N0416
Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids could represscancer cell progression
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
CWHM-12Cat No HY-18644
CWHM-12 is a potent inhibitor of withαV integrinss of 02 08 15 and 18 nM for IC50 αvβ8
and αvβ3 αvβ6 αvβ1
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK)Cat No HY-P0023
Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin with an of 094 nMα βv 3 IC50
Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK) TFACat No HY-P0023A
Cyclo(-RGDfK) TFA is a potent and selectiveinhibitor of the integrin with an ofα βv 3 IC50
094 nM Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity 9981Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
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Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat No HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof with antitumor activityintegrin αvβ3
Purity 9940Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RADfK)Cat No HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch therapy and diagnosis ofneoangiogenesis
Purity 9803Clinical Data No Development ReportedSize 1 mg
Cyclo(RGDyK)Cat No HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nMintegrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RGDyK) trifluoroacetateCat No HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
E7820 (ER68203-00) Cat No HY-14571
E7820 (ER68203-00) an orally active aromaticsulfonamide derivative is a unique angiogenesisinhibitor suppressing an expression of integrin
subunit on endothelium E7820 inhibits ratalpha2aorta angiogenesis with an of 011 μgmlIC50
Purity 9936Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
EchistatinCat No HY-P1189
Echistatin the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Echistatin TFACat No HY-P1189A
Echistatin TFA the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EptifibatideCat No HY-B0686
Eptifibatide is a cyclic heptapeptide acts as acompetitive antagonist for the activated platelet
with anti-plateletglycoprotein IIbIIIa receptoractivity
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Eptifibatide acetateCat No HY-B0686A
Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Firategrast (SB 683699) Cat No HY-14951
Firategrast (SB 683699) is an orally active andspecific antagonistα4β1α4β7 integrinFirategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) anddecreases multiple sclerosis (MS) activity
Purity 9988Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
wwwMedChemExpresscom 15
ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
wwwMedChemExpresscom 17
SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 19
Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 21
Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
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AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
wwwMedChemExpresscom 25
BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
wwwMedChemExpresscom 27
DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
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Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 51
ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
Dynamin
Dynamins are large superfamily GTPase proteins that are involved in various cellular processes including budding of transportvesicles division of organelles cytokinesis and pathogen resistance Dynamins are involved in scission (cleavage of the vesicle fromthe parent membrane) of nascent vesicles from parent membranes in eukaryotic cells Dynamins interact directly with the lipidbilayer at the necks of clathrin-coated pits to sever and release coated vesicles Dynamins contain five domains including GTPasedomain middle domain PH domain GTPase effector domain (GED) and proline rich domain (PRD) while the dynamin-relatedproteins (DRPs) lack one or more of these domains or have additional domains Dynamins and DRPs participate in a wide variety ofcellular processes including budding mitochondrial fission (mammalian Dlp1 and Dnm1) and fusionSaccharomyces cerevisiae(mammalian OPA1 Mgm1 and Msp1) vacuolar fission ( Vps1)Scerevisiae Schizosaccharomycespombe S cerevisiaeinterferon-induced anti-viral protection (fish Mx proteins) plant cell cytokinesis and membrane fission ( DRPArabidopsis thalianaproteins) as well as pathogen resistance
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Dynamin Inhibitors
Dynamin inhibitory peptideCat No HY-P1083
Dynamin inhibitory peptide competitively blocksbinding of to amphiphysin thusdynaminpreventing endocytosis Dynamin inhibitory peptideblocks the dopamine D3 effect on GABAA receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Dynamin inhibitory peptide TFACat No HY-P1083A
Dynamin inhibitory peptide TFA competitivelyblocks binding of to amphiphysin thusdynaminpreventing endocytosis Dynamin inhibitory peptideTFA blocks the dopamine D effect on GABA3 A
receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynaMin inhibitory peptide myristoylatedCat No HY-P1369
DynaMin inhibitory peptide myristoylated is a inhibitor to interfere with the bindingDynaMin
of amphiphysin with dynamin DynaMin inhibitorypeptide myristoylated is a membrane-permeant formof the peptide that prevents endocytosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynaMin inhibitory peptide myristoylated TFACat No HY-P1369A
DynaMin inhibitory peptide myristoylated TFA is a inhibitor to interfere with the bindingDynaMin
of amphiphysin with dynamin DynaMin inhibitorypeptide myristoylated TFA is a membrane-permeantform of the peptide that prevents endocytosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynasoreCat No HY-15304
Dynasore is a cell-permeable inhibitordynaminwith an of 15 μMIC50
Purity 9870Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Hydroxy-Dynasore (Dyngo-4a) Cat No HY-13863
Hydroxy Dynasore (Dyngo-4a) a structural analogof Dynasore (HY-15304) is an potency improvedlow cytotoxicity and nonspecific binding
inhibitor with values of 038dynamin IC50
μM and 23 μM for brain dynamin I andrecombinant rat dynamin II respectively
Purity 9614Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Mdivi-1 (Mitochondrial division inhibitor 1) Cat No HY-15886
Mdivi-1 is a selective dynamin-related protein 1( ) inhibitor Mdivi-1 is a mitochondrialDrp1division inhibitormitophagy
Purity 9973Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SchaftosideCat No HY-N0703
Schaftoside is a flavonoid found in a variety ofChinese herbal medicines such as Eleusine indicaSchaftoside inhibits the expression of TLR4 andMyd88 Schaftoside also decreases Drp1 expressionand phosphorylation and reduces mitochondrialfission
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 20 mg
wwwMedChemExpresscom 7
Gap Junction Protein
Gap junction channels are essential in normal heart function and they assist in the mediated spread of electrical impulses thatstimulate synchronized contraction (via an electrical syncytium) of cardiac tissues
Gap junction (GJ) proteins play an important role in direct communication between cells of many tissue types GJs are specialisedintercellular membrane-spanning domains that allow the passage of small molecules including second messenger (eg c-AMPinositol triphosphate) or ionic signals from one cell to another GJ proteins and their long evolutionary history have permittedadaptation of gap junction intercellular communication (GJIC) with several important functions and multiple regulatory processesFormation of GJIC is an essential mechanism in coordinating growth and development and tissue compartmentalization duringembryonic development
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Gap Junction Protein Inhibitors amp Modulators
AT-1002Cat No HY-114426
AT-1002 a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AT-1002 TFACat No HY-114426A
AT-1002 TFA a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Carbenoxolone disodiumCat No HY-B1367
Carbenoxolone disodium is the active metaboliteof Glycyrrhizic acid (HY-N0184) and the inhibitorof human and bacterial 11β-HSD 3α 20β-HSDCarbenoxolone disodium is an uncoupling agent for
and a potent inhibitor of gap junctions Vacciniavirus replication
Purity 9929Clinical Data LaunchedSize 10 mM times 1 mL 25 mg 50 mg 100 mg
Danegaptide (GAP-134 ZP 1609) Cat No HY-10913
Danegaptide (GAP-134) is a potent selective andorally active modifier with angap-junctionantiarrhythmic effect
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
Danegaptide Hydrochloride (GAP-134 Hydrochloride ZP 1609 Hydrochloride) Cat No HY-10913A
Danegaptide Hydrochloride (GAP-134 Hydrochloride)is a potent selective and orally active
modifier with an antiarrhythmicgap-junctioneffect
Purity 9975Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Gap 26Cat No HY-P1082
Gap 26 is a connexin mimetic peptide composed ofresidue numbers 63-75 of the first extracellularloop of connexin 43 (gap junction blocker)containing the SHVR amino acid motif
Purity 9964Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 26 TFACat No HY-P1082A
Gap 26 TFA is a connexin mimetic peptide composedof residue numbers 63-75 of the firstextracellular loop of connexin 43 (gap junctionblocker) containing the SHVR amino acid motif
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 27Cat No HY-P0139
Gap 27 a synthetic connexin43 mimetic peptide isa gap junction inhibitor Gap 27 possessesconserved sequence homology to a portion of thesecond extracellular loop leading into the fourthtransmembrane connexin segment
Purity 9807Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19Cat No HY-P1136
Gap19 a peptide derived from nine amino acids ofthe Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19 TFACat No HY-P1136A
Gap19 TFA a peptide derived from nine amino acidsof the Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 TFA inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
wwwMedChemExpresscom 9
Larazotide acetateCat No HY-106268A
Larazotide acetate is a synthetic peptideLarazotide acetate acts as a tight junctionregulator and reverses leaky junctions to theirnormally closed state
Purity 9968Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Meclofenamate sodium (Meclofenamic acid sodium) Cat No HY-B1320
Meclofenamic acid sodium is a nonsteroidalanti-inflammatory drug (NSAID) approved for use inarthritis (osteo and rheumatoid) analgesia (mildto moderate pain) dysmenorrhea and heavymenstrual blood loss (menorrhagia)
Purity 9862Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 200 mg
Meclofenamic acidCat No HY-117275
Meclofenamic Acid a non-steroidalanti-inflammatory agent is a highly selectivefat mass and obesity-associated (FTO) enzymeinhibitor Meclofenamic Acid competes with FTObinding for the m(6)A-containing nucleic acid
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Rotigaptide (ZP123) Cat No HY-106225
Rotigaptide (ZP123) is a novel and specificmodulator of Rotigaptideconnexin 43 (Cx43)prevents the uncoupling of Cx43-mediated gap
communication and normalizes cell-to-celljunctioncommunication during acute metabolic stress
Purity 9963Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg
TAT-Gap19Cat No HY-P1136B
TAT-Gap19 a Cx mimetic peptide is a specific inhibitorconnexin43 hemichannel (Cx43 HC)
TAT-Gap19 does not inhibits the corresponding Cx43GJCs TAT-Gap19 traverses the blood-brain barrierand alleviate liver fibrosis in mice
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tonabersat (SB-220453) Cat No HY-15204
Tonabersat (SB-220453) is a modulatorgap-junctionTonabersat prevents inflammatory damage in thecentral nervous system
Purity 9968Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
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Integrin
Integrins a family of heterodimeric adhesion receptors for diverse extracellular matrices have consistently been implicated ascrucial drivers of ovarian cancer development and progression A number of the RGD-based members of the integrin familyincluding α5β1 and αvβ3 or αvβ5 integrins are markedly elevated in aggressive ovarian tumors These adhesion receptors appearto promote cell adhesion survival motility and invasion during ovarian tumor growth or metastatic progression Importantly thefunctions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signalingincluding the PI3KAkt- and RasMAPK-dependent pathways
Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion Modulationof these molecules particularly αv integrin family has exhibited profound effects on fibrosis in multiple organ and disease stateBased on the several studies the integrins αvβ3 αvβ5 αvβ6 and αvβ8 have been known to modulate the fibrotic process viaactivation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis
Each integrin is typically formed by the non-covalent pairing of one α subunit of which 18 types are known to exist and one βsubunit of which 8 types are known to exist Together 24 distinct heterodimers have been identified to date The αv subunit canform heterodimers with the β1 β3 β5 β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11 andαv indicating that not all theoretically possible α and subunit pairs form Interestingly the activation of TGF-β appears to be acommon function of multiple αv integrins
wwwMedChemExpresscom 11
Integrin Inhibitors Agonists Antagonists amp Modulators
A-205804Cat No HY-100226
A-205804 is an orally bioavailable potent andselective lead inhibitor of andE-selectin
expression with an of 20 nM and 25ICAM-1 IC50
nM for E-selectin and ICAM-1 respectivelyA-205804 can be used in the research of chronicinflammatory diseases
Purity 9812Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Arg-Gly-Asp-Ser (RGDS peptide Fibronectin tetrapeptide) Cat No HY-12290
Arg-Gly-Asp-Ser is an integrin binding sequencethat inhibits functionintegrin receptordecreases systemic inflammation via inhibition ofcollagen-triggered activation of leukocytes andattenuates expression of inflammatory cytokinesiNOS and MMP-9
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Arg-Gly-Asp-Ser (TFA) (RGDS peptide (TFA) Fibronectin tetrapeptide (TFA)) Cat No HY-12290A
Arg-Gly-Asp-Ser (TFA) is an integrin bindingsequence that inhibits functionintegrin receptorArg-Gly-Asp-Ser (TFA) directly and specificallybind pro-caspase-8 pro-caspase-9 andpro-caspase-3 while it does not bindpro-caspase-1
Purity gt98Clinical DataSize 1 mg 5 mg
ATN-161 trifluoroacetate salt (ATN-161 TFA salt) Cat No HY-13535A
ATN-161 trifluoroacetate salt is a novel integrin antagonist which inhibits angiogenesis andα5β1
growth of liver metastases in a murine model
Purity ge950Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg
BI-1950Cat No HY-124040
BI-1950 is a highly potent lymphocyte function inhibitor LFA-1 isassociated antigen-1 (LFA-1)
an essential component in normal immune systemfunction and a target for drug discovery
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO-1211Cat No HY-14126
BIO-1211 is a highly selective and orally active inhibitor with values of 4 nMα4β1 (VLA-4) IC50
and 2 μM for α4β1 and α4β7 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192Cat No HY-107589
BIO5192 is a selective and potent integrin α4β1(VLA-4) inhibitor ( lt10 pM) BIO5192Kd
selectively binds to α4β1 ( =18 nM) over aIC50
range of other integrins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192 hydrateCat No HY-107589A
BIO5192 hydrate is a selective and potent integrin inhibitor ( lt10 pM) BIO5192α4β1 (VLA-4) Kd
hydrate selectively binds to α4β1 ( =18 nM)IC50
over a range of other integrins
Purity ge980Clinical Data No Development ReportedSize 1 mg
BMS-688521Cat No HY-10596
BMS-688521 is a highly potent orally activeinhibitor of the interaction withLFA-1ICAMan of 25 nM in the adhesion assay and anIC50
of 60 nM in the MLR assay BMS-688521 isIC50
efficacious in a mouse allergic eosinophilic lunginflammation model
Purity 9925Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
BOP sodiumCat No HY-129453
BOP sodium is a potent and selective dual inhibitor with values inα9β1α4β1 integrin Kd
the picomolar range BOP sodium shows the rapidand preferential mobilization of hematopoieticstem cell (HSC) and progenitors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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c(phg-isoDGR-(NMe)k)Cat No HY-111413
c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
c(phg-isoDGR-(NMe)k) TFACat No HY-111413A
c(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
CarotegrastCat No HY-14857
Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor
activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Carotegrast methyl (AJM300) Cat No HY-124290
Carotegrast methyl (AJM300) is an orally activeand selective antagonist HCA2969 anα4 integrinactive metabolite of AJM300 is a specific dualα4β1α4β7 integrin antagonist Carotegrast methylprevents the development of colitis in miceltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cilengitide (EMD 121974) Cat No HY-16141
Cilengitide (EMD 121974) is a potent and selectiveinhibitor of the and integrins α βν 3 α βν 5
Cilengitide inhibits binding of isolated α βν 3
and α β to Vitronectin with an IC value of 4ν 5 50
and 79 nM respectively
Purity 9932Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cilengitide TFA (EMD 121974 TFA) Cat No HY-16143
Cilengitide is a potent and selective integrininhibitor for α β and α β receptor withv 3 v 5
values of 4 nM and 79 nM respectivelyIC50
Purity 9885Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Cucurbitacin BCat No HY-N0416
Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids could represscancer cell progression
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
CWHM-12Cat No HY-18644
CWHM-12 is a potent inhibitor of withαV integrinss of 02 08 15 and 18 nM for IC50 αvβ8
and αvβ3 αvβ6 αvβ1
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK)Cat No HY-P0023
Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin with an of 094 nMα βv 3 IC50
Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK) TFACat No HY-P0023A
Cyclo(-RGDfK) TFA is a potent and selectiveinhibitor of the integrin with an ofα βv 3 IC50
094 nM Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity 9981Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
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Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat No HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof with antitumor activityintegrin αvβ3
Purity 9940Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RADfK)Cat No HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch therapy and diagnosis ofneoangiogenesis
Purity 9803Clinical Data No Development ReportedSize 1 mg
Cyclo(RGDyK)Cat No HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nMintegrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RGDyK) trifluoroacetateCat No HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
E7820 (ER68203-00) Cat No HY-14571
E7820 (ER68203-00) an orally active aromaticsulfonamide derivative is a unique angiogenesisinhibitor suppressing an expression of integrin
subunit on endothelium E7820 inhibits ratalpha2aorta angiogenesis with an of 011 μgmlIC50
Purity 9936Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
EchistatinCat No HY-P1189
Echistatin the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Echistatin TFACat No HY-P1189A
Echistatin TFA the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EptifibatideCat No HY-B0686
Eptifibatide is a cyclic heptapeptide acts as acompetitive antagonist for the activated platelet
with anti-plateletglycoprotein IIbIIIa receptoractivity
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Eptifibatide acetateCat No HY-B0686A
Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Firategrast (SB 683699) Cat No HY-14951
Firategrast (SB 683699) is an orally active andspecific antagonistα4β1α4β7 integrinFirategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) anddecreases multiple sclerosis (MS) activity
Purity 9988Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
wwwMedChemExpresscom 15
ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
wwwMedChemExpresscom 17
SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 19
Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 21
Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
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AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
wwwMedChemExpresscom 25
BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
wwwMedChemExpresscom 27
DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 35
Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
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Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 51
ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
Dynamin Inhibitors
Dynamin inhibitory peptideCat No HY-P1083
Dynamin inhibitory peptide competitively blocksbinding of to amphiphysin thusdynaminpreventing endocytosis Dynamin inhibitory peptideblocks the dopamine D3 effect on GABAA receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Dynamin inhibitory peptide TFACat No HY-P1083A
Dynamin inhibitory peptide TFA competitivelyblocks binding of to amphiphysin thusdynaminpreventing endocytosis Dynamin inhibitory peptideTFA blocks the dopamine D effect on GABA3 A
receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynaMin inhibitory peptide myristoylatedCat No HY-P1369
DynaMin inhibitory peptide myristoylated is a inhibitor to interfere with the bindingDynaMin
of amphiphysin with dynamin DynaMin inhibitorypeptide myristoylated is a membrane-permeant formof the peptide that prevents endocytosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynaMin inhibitory peptide myristoylated TFACat No HY-P1369A
DynaMin inhibitory peptide myristoylated TFA is a inhibitor to interfere with the bindingDynaMin
of amphiphysin with dynamin DynaMin inhibitorypeptide myristoylated TFA is a membrane-permeantform of the peptide that prevents endocytosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
DynasoreCat No HY-15304
Dynasore is a cell-permeable inhibitordynaminwith an of 15 μMIC50
Purity 9870Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Hydroxy-Dynasore (Dyngo-4a) Cat No HY-13863
Hydroxy Dynasore (Dyngo-4a) a structural analogof Dynasore (HY-15304) is an potency improvedlow cytotoxicity and nonspecific binding
inhibitor with values of 038dynamin IC50
μM and 23 μM for brain dynamin I andrecombinant rat dynamin II respectively
Purity 9614Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Mdivi-1 (Mitochondrial division inhibitor 1) Cat No HY-15886
Mdivi-1 is a selective dynamin-related protein 1( ) inhibitor Mdivi-1 is a mitochondrialDrp1division inhibitormitophagy
Purity 9973Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SchaftosideCat No HY-N0703
Schaftoside is a flavonoid found in a variety ofChinese herbal medicines such as Eleusine indicaSchaftoside inhibits the expression of TLR4 andMyd88 Schaftoside also decreases Drp1 expressionand phosphorylation and reduces mitochondrialfission
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 20 mg
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Gap Junction Protein
Gap junction channels are essential in normal heart function and they assist in the mediated spread of electrical impulses thatstimulate synchronized contraction (via an electrical syncytium) of cardiac tissues
Gap junction (GJ) proteins play an important role in direct communication between cells of many tissue types GJs are specialisedintercellular membrane-spanning domains that allow the passage of small molecules including second messenger (eg c-AMPinositol triphosphate) or ionic signals from one cell to another GJ proteins and their long evolutionary history have permittedadaptation of gap junction intercellular communication (GJIC) with several important functions and multiple regulatory processesFormation of GJIC is an essential mechanism in coordinating growth and development and tissue compartmentalization duringembryonic development
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Gap Junction Protein Inhibitors amp Modulators
AT-1002Cat No HY-114426
AT-1002 a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AT-1002 TFACat No HY-114426A
AT-1002 TFA a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Carbenoxolone disodiumCat No HY-B1367
Carbenoxolone disodium is the active metaboliteof Glycyrrhizic acid (HY-N0184) and the inhibitorof human and bacterial 11β-HSD 3α 20β-HSDCarbenoxolone disodium is an uncoupling agent for
and a potent inhibitor of gap junctions Vacciniavirus replication
Purity 9929Clinical Data LaunchedSize 10 mM times 1 mL 25 mg 50 mg 100 mg
Danegaptide (GAP-134 ZP 1609) Cat No HY-10913
Danegaptide (GAP-134) is a potent selective andorally active modifier with angap-junctionantiarrhythmic effect
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
Danegaptide Hydrochloride (GAP-134 Hydrochloride ZP 1609 Hydrochloride) Cat No HY-10913A
Danegaptide Hydrochloride (GAP-134 Hydrochloride)is a potent selective and orally active
modifier with an antiarrhythmicgap-junctioneffect
Purity 9975Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Gap 26Cat No HY-P1082
Gap 26 is a connexin mimetic peptide composed ofresidue numbers 63-75 of the first extracellularloop of connexin 43 (gap junction blocker)containing the SHVR amino acid motif
Purity 9964Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 26 TFACat No HY-P1082A
Gap 26 TFA is a connexin mimetic peptide composedof residue numbers 63-75 of the firstextracellular loop of connexin 43 (gap junctionblocker) containing the SHVR amino acid motif
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 27Cat No HY-P0139
Gap 27 a synthetic connexin43 mimetic peptide isa gap junction inhibitor Gap 27 possessesconserved sequence homology to a portion of thesecond extracellular loop leading into the fourthtransmembrane connexin segment
Purity 9807Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19Cat No HY-P1136
Gap19 a peptide derived from nine amino acids ofthe Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19 TFACat No HY-P1136A
Gap19 TFA a peptide derived from nine amino acidsof the Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 TFA inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
wwwMedChemExpresscom 9
Larazotide acetateCat No HY-106268A
Larazotide acetate is a synthetic peptideLarazotide acetate acts as a tight junctionregulator and reverses leaky junctions to theirnormally closed state
Purity 9968Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Meclofenamate sodium (Meclofenamic acid sodium) Cat No HY-B1320
Meclofenamic acid sodium is a nonsteroidalanti-inflammatory drug (NSAID) approved for use inarthritis (osteo and rheumatoid) analgesia (mildto moderate pain) dysmenorrhea and heavymenstrual blood loss (menorrhagia)
Purity 9862Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 200 mg
Meclofenamic acidCat No HY-117275
Meclofenamic Acid a non-steroidalanti-inflammatory agent is a highly selectivefat mass and obesity-associated (FTO) enzymeinhibitor Meclofenamic Acid competes with FTObinding for the m(6)A-containing nucleic acid
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Rotigaptide (ZP123) Cat No HY-106225
Rotigaptide (ZP123) is a novel and specificmodulator of Rotigaptideconnexin 43 (Cx43)prevents the uncoupling of Cx43-mediated gap
communication and normalizes cell-to-celljunctioncommunication during acute metabolic stress
Purity 9963Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg
TAT-Gap19Cat No HY-P1136B
TAT-Gap19 a Cx mimetic peptide is a specific inhibitorconnexin43 hemichannel (Cx43 HC)
TAT-Gap19 does not inhibits the corresponding Cx43GJCs TAT-Gap19 traverses the blood-brain barrierand alleviate liver fibrosis in mice
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tonabersat (SB-220453) Cat No HY-15204
Tonabersat (SB-220453) is a modulatorgap-junctionTonabersat prevents inflammatory damage in thecentral nervous system
Purity 9968Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
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Integrin
Integrins a family of heterodimeric adhesion receptors for diverse extracellular matrices have consistently been implicated ascrucial drivers of ovarian cancer development and progression A number of the RGD-based members of the integrin familyincluding α5β1 and αvβ3 or αvβ5 integrins are markedly elevated in aggressive ovarian tumors These adhesion receptors appearto promote cell adhesion survival motility and invasion during ovarian tumor growth or metastatic progression Importantly thefunctions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signalingincluding the PI3KAkt- and RasMAPK-dependent pathways
Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion Modulationof these molecules particularly αv integrin family has exhibited profound effects on fibrosis in multiple organ and disease stateBased on the several studies the integrins αvβ3 αvβ5 αvβ6 and αvβ8 have been known to modulate the fibrotic process viaactivation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis
Each integrin is typically formed by the non-covalent pairing of one α subunit of which 18 types are known to exist and one βsubunit of which 8 types are known to exist Together 24 distinct heterodimers have been identified to date The αv subunit canform heterodimers with the β1 β3 β5 β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11 andαv indicating that not all theoretically possible α and subunit pairs form Interestingly the activation of TGF-β appears to be acommon function of multiple αv integrins
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Integrin Inhibitors Agonists Antagonists amp Modulators
A-205804Cat No HY-100226
A-205804 is an orally bioavailable potent andselective lead inhibitor of andE-selectin
expression with an of 20 nM and 25ICAM-1 IC50
nM for E-selectin and ICAM-1 respectivelyA-205804 can be used in the research of chronicinflammatory diseases
Purity 9812Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Arg-Gly-Asp-Ser (RGDS peptide Fibronectin tetrapeptide) Cat No HY-12290
Arg-Gly-Asp-Ser is an integrin binding sequencethat inhibits functionintegrin receptordecreases systemic inflammation via inhibition ofcollagen-triggered activation of leukocytes andattenuates expression of inflammatory cytokinesiNOS and MMP-9
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Arg-Gly-Asp-Ser (TFA) (RGDS peptide (TFA) Fibronectin tetrapeptide (TFA)) Cat No HY-12290A
Arg-Gly-Asp-Ser (TFA) is an integrin bindingsequence that inhibits functionintegrin receptorArg-Gly-Asp-Ser (TFA) directly and specificallybind pro-caspase-8 pro-caspase-9 andpro-caspase-3 while it does not bindpro-caspase-1
Purity gt98Clinical DataSize 1 mg 5 mg
ATN-161 trifluoroacetate salt (ATN-161 TFA salt) Cat No HY-13535A
ATN-161 trifluoroacetate salt is a novel integrin antagonist which inhibits angiogenesis andα5β1
growth of liver metastases in a murine model
Purity ge950Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg
BI-1950Cat No HY-124040
BI-1950 is a highly potent lymphocyte function inhibitor LFA-1 isassociated antigen-1 (LFA-1)
an essential component in normal immune systemfunction and a target for drug discovery
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO-1211Cat No HY-14126
BIO-1211 is a highly selective and orally active inhibitor with values of 4 nMα4β1 (VLA-4) IC50
and 2 μM for α4β1 and α4β7 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192Cat No HY-107589
BIO5192 is a selective and potent integrin α4β1(VLA-4) inhibitor ( lt10 pM) BIO5192Kd
selectively binds to α4β1 ( =18 nM) over aIC50
range of other integrins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192 hydrateCat No HY-107589A
BIO5192 hydrate is a selective and potent integrin inhibitor ( lt10 pM) BIO5192α4β1 (VLA-4) Kd
hydrate selectively binds to α4β1 ( =18 nM)IC50
over a range of other integrins
Purity ge980Clinical Data No Development ReportedSize 1 mg
BMS-688521Cat No HY-10596
BMS-688521 is a highly potent orally activeinhibitor of the interaction withLFA-1ICAMan of 25 nM in the adhesion assay and anIC50
of 60 nM in the MLR assay BMS-688521 isIC50
efficacious in a mouse allergic eosinophilic lunginflammation model
Purity 9925Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
BOP sodiumCat No HY-129453
BOP sodium is a potent and selective dual inhibitor with values inα9β1α4β1 integrin Kd
the picomolar range BOP sodium shows the rapidand preferential mobilization of hematopoieticstem cell (HSC) and progenitors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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c(phg-isoDGR-(NMe)k)Cat No HY-111413
c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
c(phg-isoDGR-(NMe)k) TFACat No HY-111413A
c(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
CarotegrastCat No HY-14857
Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor
activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Carotegrast methyl (AJM300) Cat No HY-124290
Carotegrast methyl (AJM300) is an orally activeand selective antagonist HCA2969 anα4 integrinactive metabolite of AJM300 is a specific dualα4β1α4β7 integrin antagonist Carotegrast methylprevents the development of colitis in miceltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cilengitide (EMD 121974) Cat No HY-16141
Cilengitide (EMD 121974) is a potent and selectiveinhibitor of the and integrins α βν 3 α βν 5
Cilengitide inhibits binding of isolated α βν 3
and α β to Vitronectin with an IC value of 4ν 5 50
and 79 nM respectively
Purity 9932Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cilengitide TFA (EMD 121974 TFA) Cat No HY-16143
Cilengitide is a potent and selective integrininhibitor for α β and α β receptor withv 3 v 5
values of 4 nM and 79 nM respectivelyIC50
Purity 9885Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Cucurbitacin BCat No HY-N0416
Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids could represscancer cell progression
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
CWHM-12Cat No HY-18644
CWHM-12 is a potent inhibitor of withαV integrinss of 02 08 15 and 18 nM for IC50 αvβ8
and αvβ3 αvβ6 αvβ1
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK)Cat No HY-P0023
Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin with an of 094 nMα βv 3 IC50
Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK) TFACat No HY-P0023A
Cyclo(-RGDfK) TFA is a potent and selectiveinhibitor of the integrin with an ofα βv 3 IC50
094 nM Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity 9981Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
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Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat No HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof with antitumor activityintegrin αvβ3
Purity 9940Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RADfK)Cat No HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch therapy and diagnosis ofneoangiogenesis
Purity 9803Clinical Data No Development ReportedSize 1 mg
Cyclo(RGDyK)Cat No HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nMintegrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RGDyK) trifluoroacetateCat No HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
E7820 (ER68203-00) Cat No HY-14571
E7820 (ER68203-00) an orally active aromaticsulfonamide derivative is a unique angiogenesisinhibitor suppressing an expression of integrin
subunit on endothelium E7820 inhibits ratalpha2aorta angiogenesis with an of 011 μgmlIC50
Purity 9936Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
EchistatinCat No HY-P1189
Echistatin the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Echistatin TFACat No HY-P1189A
Echistatin TFA the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EptifibatideCat No HY-B0686
Eptifibatide is a cyclic heptapeptide acts as acompetitive antagonist for the activated platelet
with anti-plateletglycoprotein IIbIIIa receptoractivity
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Eptifibatide acetateCat No HY-B0686A
Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Firategrast (SB 683699) Cat No HY-14951
Firategrast (SB 683699) is an orally active andspecific antagonistα4β1α4β7 integrinFirategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) anddecreases multiple sclerosis (MS) activity
Purity 9988Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
wwwMedChemExpresscom 15
ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
wwwMedChemExpresscom 17
SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 19
Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 21
Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
24 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
wwwMedChemExpresscom 25
BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
wwwMedChemExpresscom 27
DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 35
Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
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Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 51
ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
Gap Junction Protein
Gap junction channels are essential in normal heart function and they assist in the mediated spread of electrical impulses thatstimulate synchronized contraction (via an electrical syncytium) of cardiac tissues
Gap junction (GJ) proteins play an important role in direct communication between cells of many tissue types GJs are specialisedintercellular membrane-spanning domains that allow the passage of small molecules including second messenger (eg c-AMPinositol triphosphate) or ionic signals from one cell to another GJ proteins and their long evolutionary history have permittedadaptation of gap junction intercellular communication (GJIC) with several important functions and multiple regulatory processesFormation of GJIC is an essential mechanism in coordinating growth and development and tissue compartmentalization duringembryonic development
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Gap Junction Protein Inhibitors amp Modulators
AT-1002Cat No HY-114426
AT-1002 a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AT-1002 TFACat No HY-114426A
AT-1002 TFA a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Carbenoxolone disodiumCat No HY-B1367
Carbenoxolone disodium is the active metaboliteof Glycyrrhizic acid (HY-N0184) and the inhibitorof human and bacterial 11β-HSD 3α 20β-HSDCarbenoxolone disodium is an uncoupling agent for
and a potent inhibitor of gap junctions Vacciniavirus replication
Purity 9929Clinical Data LaunchedSize 10 mM times 1 mL 25 mg 50 mg 100 mg
Danegaptide (GAP-134 ZP 1609) Cat No HY-10913
Danegaptide (GAP-134) is a potent selective andorally active modifier with angap-junctionantiarrhythmic effect
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
Danegaptide Hydrochloride (GAP-134 Hydrochloride ZP 1609 Hydrochloride) Cat No HY-10913A
Danegaptide Hydrochloride (GAP-134 Hydrochloride)is a potent selective and orally active
modifier with an antiarrhythmicgap-junctioneffect
Purity 9975Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Gap 26Cat No HY-P1082
Gap 26 is a connexin mimetic peptide composed ofresidue numbers 63-75 of the first extracellularloop of connexin 43 (gap junction blocker)containing the SHVR amino acid motif
Purity 9964Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 26 TFACat No HY-P1082A
Gap 26 TFA is a connexin mimetic peptide composedof residue numbers 63-75 of the firstextracellular loop of connexin 43 (gap junctionblocker) containing the SHVR amino acid motif
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 27Cat No HY-P0139
Gap 27 a synthetic connexin43 mimetic peptide isa gap junction inhibitor Gap 27 possessesconserved sequence homology to a portion of thesecond extracellular loop leading into the fourthtransmembrane connexin segment
Purity 9807Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19Cat No HY-P1136
Gap19 a peptide derived from nine amino acids ofthe Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19 TFACat No HY-P1136A
Gap19 TFA a peptide derived from nine amino acidsof the Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 TFA inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
wwwMedChemExpresscom 9
Larazotide acetateCat No HY-106268A
Larazotide acetate is a synthetic peptideLarazotide acetate acts as a tight junctionregulator and reverses leaky junctions to theirnormally closed state
Purity 9968Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Meclofenamate sodium (Meclofenamic acid sodium) Cat No HY-B1320
Meclofenamic acid sodium is a nonsteroidalanti-inflammatory drug (NSAID) approved for use inarthritis (osteo and rheumatoid) analgesia (mildto moderate pain) dysmenorrhea and heavymenstrual blood loss (menorrhagia)
Purity 9862Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 200 mg
Meclofenamic acidCat No HY-117275
Meclofenamic Acid a non-steroidalanti-inflammatory agent is a highly selectivefat mass and obesity-associated (FTO) enzymeinhibitor Meclofenamic Acid competes with FTObinding for the m(6)A-containing nucleic acid
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Rotigaptide (ZP123) Cat No HY-106225
Rotigaptide (ZP123) is a novel and specificmodulator of Rotigaptideconnexin 43 (Cx43)prevents the uncoupling of Cx43-mediated gap
communication and normalizes cell-to-celljunctioncommunication during acute metabolic stress
Purity 9963Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg
TAT-Gap19Cat No HY-P1136B
TAT-Gap19 a Cx mimetic peptide is a specific inhibitorconnexin43 hemichannel (Cx43 HC)
TAT-Gap19 does not inhibits the corresponding Cx43GJCs TAT-Gap19 traverses the blood-brain barrierand alleviate liver fibrosis in mice
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tonabersat (SB-220453) Cat No HY-15204
Tonabersat (SB-220453) is a modulatorgap-junctionTonabersat prevents inflammatory damage in thecentral nervous system
Purity 9968Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
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Integrin
Integrins a family of heterodimeric adhesion receptors for diverse extracellular matrices have consistently been implicated ascrucial drivers of ovarian cancer development and progression A number of the RGD-based members of the integrin familyincluding α5β1 and αvβ3 or αvβ5 integrins are markedly elevated in aggressive ovarian tumors These adhesion receptors appearto promote cell adhesion survival motility and invasion during ovarian tumor growth or metastatic progression Importantly thefunctions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signalingincluding the PI3KAkt- and RasMAPK-dependent pathways
Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion Modulationof these molecules particularly αv integrin family has exhibited profound effects on fibrosis in multiple organ and disease stateBased on the several studies the integrins αvβ3 αvβ5 αvβ6 and αvβ8 have been known to modulate the fibrotic process viaactivation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis
Each integrin is typically formed by the non-covalent pairing of one α subunit of which 18 types are known to exist and one βsubunit of which 8 types are known to exist Together 24 distinct heterodimers have been identified to date The αv subunit canform heterodimers with the β1 β3 β5 β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11 andαv indicating that not all theoretically possible α and subunit pairs form Interestingly the activation of TGF-β appears to be acommon function of multiple αv integrins
wwwMedChemExpresscom 11
Integrin Inhibitors Agonists Antagonists amp Modulators
A-205804Cat No HY-100226
A-205804 is an orally bioavailable potent andselective lead inhibitor of andE-selectin
expression with an of 20 nM and 25ICAM-1 IC50
nM for E-selectin and ICAM-1 respectivelyA-205804 can be used in the research of chronicinflammatory diseases
Purity 9812Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Arg-Gly-Asp-Ser (RGDS peptide Fibronectin tetrapeptide) Cat No HY-12290
Arg-Gly-Asp-Ser is an integrin binding sequencethat inhibits functionintegrin receptordecreases systemic inflammation via inhibition ofcollagen-triggered activation of leukocytes andattenuates expression of inflammatory cytokinesiNOS and MMP-9
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Arg-Gly-Asp-Ser (TFA) (RGDS peptide (TFA) Fibronectin tetrapeptide (TFA)) Cat No HY-12290A
Arg-Gly-Asp-Ser (TFA) is an integrin bindingsequence that inhibits functionintegrin receptorArg-Gly-Asp-Ser (TFA) directly and specificallybind pro-caspase-8 pro-caspase-9 andpro-caspase-3 while it does not bindpro-caspase-1
Purity gt98Clinical DataSize 1 mg 5 mg
ATN-161 trifluoroacetate salt (ATN-161 TFA salt) Cat No HY-13535A
ATN-161 trifluoroacetate salt is a novel integrin antagonist which inhibits angiogenesis andα5β1
growth of liver metastases in a murine model
Purity ge950Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg
BI-1950Cat No HY-124040
BI-1950 is a highly potent lymphocyte function inhibitor LFA-1 isassociated antigen-1 (LFA-1)
an essential component in normal immune systemfunction and a target for drug discovery
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO-1211Cat No HY-14126
BIO-1211 is a highly selective and orally active inhibitor with values of 4 nMα4β1 (VLA-4) IC50
and 2 μM for α4β1 and α4β7 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192Cat No HY-107589
BIO5192 is a selective and potent integrin α4β1(VLA-4) inhibitor ( lt10 pM) BIO5192Kd
selectively binds to α4β1 ( =18 nM) over aIC50
range of other integrins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192 hydrateCat No HY-107589A
BIO5192 hydrate is a selective and potent integrin inhibitor ( lt10 pM) BIO5192α4β1 (VLA-4) Kd
hydrate selectively binds to α4β1 ( =18 nM)IC50
over a range of other integrins
Purity ge980Clinical Data No Development ReportedSize 1 mg
BMS-688521Cat No HY-10596
BMS-688521 is a highly potent orally activeinhibitor of the interaction withLFA-1ICAMan of 25 nM in the adhesion assay and anIC50
of 60 nM in the MLR assay BMS-688521 isIC50
efficacious in a mouse allergic eosinophilic lunginflammation model
Purity 9925Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
BOP sodiumCat No HY-129453
BOP sodium is a potent and selective dual inhibitor with values inα9β1α4β1 integrin Kd
the picomolar range BOP sodium shows the rapidand preferential mobilization of hematopoieticstem cell (HSC) and progenitors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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c(phg-isoDGR-(NMe)k)Cat No HY-111413
c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
c(phg-isoDGR-(NMe)k) TFACat No HY-111413A
c(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
CarotegrastCat No HY-14857
Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor
activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Carotegrast methyl (AJM300) Cat No HY-124290
Carotegrast methyl (AJM300) is an orally activeand selective antagonist HCA2969 anα4 integrinactive metabolite of AJM300 is a specific dualα4β1α4β7 integrin antagonist Carotegrast methylprevents the development of colitis in miceltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cilengitide (EMD 121974) Cat No HY-16141
Cilengitide (EMD 121974) is a potent and selectiveinhibitor of the and integrins α βν 3 α βν 5
Cilengitide inhibits binding of isolated α βν 3
and α β to Vitronectin with an IC value of 4ν 5 50
and 79 nM respectively
Purity 9932Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cilengitide TFA (EMD 121974 TFA) Cat No HY-16143
Cilengitide is a potent and selective integrininhibitor for α β and α β receptor withv 3 v 5
values of 4 nM and 79 nM respectivelyIC50
Purity 9885Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Cucurbitacin BCat No HY-N0416
Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids could represscancer cell progression
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
CWHM-12Cat No HY-18644
CWHM-12 is a potent inhibitor of withαV integrinss of 02 08 15 and 18 nM for IC50 αvβ8
and αvβ3 αvβ6 αvβ1
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK)Cat No HY-P0023
Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin with an of 094 nMα βv 3 IC50
Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK) TFACat No HY-P0023A
Cyclo(-RGDfK) TFA is a potent and selectiveinhibitor of the integrin with an ofα βv 3 IC50
094 nM Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity 9981Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
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Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat No HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof with antitumor activityintegrin αvβ3
Purity 9940Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RADfK)Cat No HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch therapy and diagnosis ofneoangiogenesis
Purity 9803Clinical Data No Development ReportedSize 1 mg
Cyclo(RGDyK)Cat No HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nMintegrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RGDyK) trifluoroacetateCat No HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
E7820 (ER68203-00) Cat No HY-14571
E7820 (ER68203-00) an orally active aromaticsulfonamide derivative is a unique angiogenesisinhibitor suppressing an expression of integrin
subunit on endothelium E7820 inhibits ratalpha2aorta angiogenesis with an of 011 μgmlIC50
Purity 9936Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
EchistatinCat No HY-P1189
Echistatin the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Echistatin TFACat No HY-P1189A
Echistatin TFA the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EptifibatideCat No HY-B0686
Eptifibatide is a cyclic heptapeptide acts as acompetitive antagonist for the activated platelet
with anti-plateletglycoprotein IIbIIIa receptoractivity
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Eptifibatide acetateCat No HY-B0686A
Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Firategrast (SB 683699) Cat No HY-14951
Firategrast (SB 683699) is an orally active andspecific antagonistα4β1α4β7 integrinFirategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) anddecreases multiple sclerosis (MS) activity
Purity 9988Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
wwwMedChemExpresscom 15
ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
wwwMedChemExpresscom 17
SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
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Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
24 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
wwwMedChemExpresscom 25
BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
wwwMedChemExpresscom 27
DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 35
Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
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Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 51
ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
Gap Junction Protein Inhibitors amp Modulators
AT-1002Cat No HY-114426
AT-1002 a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AT-1002 TFACat No HY-114426A
AT-1002 TFA a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Carbenoxolone disodiumCat No HY-B1367
Carbenoxolone disodium is the active metaboliteof Glycyrrhizic acid (HY-N0184) and the inhibitorof human and bacterial 11β-HSD 3α 20β-HSDCarbenoxolone disodium is an uncoupling agent for
and a potent inhibitor of gap junctions Vacciniavirus replication
Purity 9929Clinical Data LaunchedSize 10 mM times 1 mL 25 mg 50 mg 100 mg
Danegaptide (GAP-134 ZP 1609) Cat No HY-10913
Danegaptide (GAP-134) is a potent selective andorally active modifier with angap-junctionantiarrhythmic effect
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
Danegaptide Hydrochloride (GAP-134 Hydrochloride ZP 1609 Hydrochloride) Cat No HY-10913A
Danegaptide Hydrochloride (GAP-134 Hydrochloride)is a potent selective and orally active
modifier with an antiarrhythmicgap-junctioneffect
Purity 9975Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Gap 26Cat No HY-P1082
Gap 26 is a connexin mimetic peptide composed ofresidue numbers 63-75 of the first extracellularloop of connexin 43 (gap junction blocker)containing the SHVR amino acid motif
Purity 9964Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 26 TFACat No HY-P1082A
Gap 26 TFA is a connexin mimetic peptide composedof residue numbers 63-75 of the firstextracellular loop of connexin 43 (gap junctionblocker) containing the SHVR amino acid motif
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Gap 27Cat No HY-P0139
Gap 27 a synthetic connexin43 mimetic peptide isa gap junction inhibitor Gap 27 possessesconserved sequence homology to a portion of thesecond extracellular loop leading into the fourthtransmembrane connexin segment
Purity 9807Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19Cat No HY-P1136
Gap19 a peptide derived from nine amino acids ofthe Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Gap19 TFACat No HY-P1136A
Gap19 TFA a peptide derived from nine amino acidsof the Cx43 cytoplasmic loop (CL) is a potent andselective connexin 43 (Cx43) hemichannelblocker Gap19 TFA inhibits hemichannels caused bypreventing intramolecular interactions of theC-terminus (CT) with the CL
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
wwwMedChemExpresscom 9
Larazotide acetateCat No HY-106268A
Larazotide acetate is a synthetic peptideLarazotide acetate acts as a tight junctionregulator and reverses leaky junctions to theirnormally closed state
Purity 9968Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Meclofenamate sodium (Meclofenamic acid sodium) Cat No HY-B1320
Meclofenamic acid sodium is a nonsteroidalanti-inflammatory drug (NSAID) approved for use inarthritis (osteo and rheumatoid) analgesia (mildto moderate pain) dysmenorrhea and heavymenstrual blood loss (menorrhagia)
Purity 9862Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 200 mg
Meclofenamic acidCat No HY-117275
Meclofenamic Acid a non-steroidalanti-inflammatory agent is a highly selectivefat mass and obesity-associated (FTO) enzymeinhibitor Meclofenamic Acid competes with FTObinding for the m(6)A-containing nucleic acid
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Rotigaptide (ZP123) Cat No HY-106225
Rotigaptide (ZP123) is a novel and specificmodulator of Rotigaptideconnexin 43 (Cx43)prevents the uncoupling of Cx43-mediated gap
communication and normalizes cell-to-celljunctioncommunication during acute metabolic stress
Purity 9963Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg
TAT-Gap19Cat No HY-P1136B
TAT-Gap19 a Cx mimetic peptide is a specific inhibitorconnexin43 hemichannel (Cx43 HC)
TAT-Gap19 does not inhibits the corresponding Cx43GJCs TAT-Gap19 traverses the blood-brain barrierand alleviate liver fibrosis in mice
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tonabersat (SB-220453) Cat No HY-15204
Tonabersat (SB-220453) is a modulatorgap-junctionTonabersat prevents inflammatory damage in thecentral nervous system
Purity 9968Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
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Integrin
Integrins a family of heterodimeric adhesion receptors for diverse extracellular matrices have consistently been implicated ascrucial drivers of ovarian cancer development and progression A number of the RGD-based members of the integrin familyincluding α5β1 and αvβ3 or αvβ5 integrins are markedly elevated in aggressive ovarian tumors These adhesion receptors appearto promote cell adhesion survival motility and invasion during ovarian tumor growth or metastatic progression Importantly thefunctions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signalingincluding the PI3KAkt- and RasMAPK-dependent pathways
Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion Modulationof these molecules particularly αv integrin family has exhibited profound effects on fibrosis in multiple organ and disease stateBased on the several studies the integrins αvβ3 αvβ5 αvβ6 and αvβ8 have been known to modulate the fibrotic process viaactivation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis
Each integrin is typically formed by the non-covalent pairing of one α subunit of which 18 types are known to exist and one βsubunit of which 8 types are known to exist Together 24 distinct heterodimers have been identified to date The αv subunit canform heterodimers with the β1 β3 β5 β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11 andαv indicating that not all theoretically possible α and subunit pairs form Interestingly the activation of TGF-β appears to be acommon function of multiple αv integrins
wwwMedChemExpresscom 11
Integrin Inhibitors Agonists Antagonists amp Modulators
A-205804Cat No HY-100226
A-205804 is an orally bioavailable potent andselective lead inhibitor of andE-selectin
expression with an of 20 nM and 25ICAM-1 IC50
nM for E-selectin and ICAM-1 respectivelyA-205804 can be used in the research of chronicinflammatory diseases
Purity 9812Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Arg-Gly-Asp-Ser (RGDS peptide Fibronectin tetrapeptide) Cat No HY-12290
Arg-Gly-Asp-Ser is an integrin binding sequencethat inhibits functionintegrin receptordecreases systemic inflammation via inhibition ofcollagen-triggered activation of leukocytes andattenuates expression of inflammatory cytokinesiNOS and MMP-9
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Arg-Gly-Asp-Ser (TFA) (RGDS peptide (TFA) Fibronectin tetrapeptide (TFA)) Cat No HY-12290A
Arg-Gly-Asp-Ser (TFA) is an integrin bindingsequence that inhibits functionintegrin receptorArg-Gly-Asp-Ser (TFA) directly and specificallybind pro-caspase-8 pro-caspase-9 andpro-caspase-3 while it does not bindpro-caspase-1
Purity gt98Clinical DataSize 1 mg 5 mg
ATN-161 trifluoroacetate salt (ATN-161 TFA salt) Cat No HY-13535A
ATN-161 trifluoroacetate salt is a novel integrin antagonist which inhibits angiogenesis andα5β1
growth of liver metastases in a murine model
Purity ge950Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg
BI-1950Cat No HY-124040
BI-1950 is a highly potent lymphocyte function inhibitor LFA-1 isassociated antigen-1 (LFA-1)
an essential component in normal immune systemfunction and a target for drug discovery
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO-1211Cat No HY-14126
BIO-1211 is a highly selective and orally active inhibitor with values of 4 nMα4β1 (VLA-4) IC50
and 2 μM for α4β1 and α4β7 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192Cat No HY-107589
BIO5192 is a selective and potent integrin α4β1(VLA-4) inhibitor ( lt10 pM) BIO5192Kd
selectively binds to α4β1 ( =18 nM) over aIC50
range of other integrins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192 hydrateCat No HY-107589A
BIO5192 hydrate is a selective and potent integrin inhibitor ( lt10 pM) BIO5192α4β1 (VLA-4) Kd
hydrate selectively binds to α4β1 ( =18 nM)IC50
over a range of other integrins
Purity ge980Clinical Data No Development ReportedSize 1 mg
BMS-688521Cat No HY-10596
BMS-688521 is a highly potent orally activeinhibitor of the interaction withLFA-1ICAMan of 25 nM in the adhesion assay and anIC50
of 60 nM in the MLR assay BMS-688521 isIC50
efficacious in a mouse allergic eosinophilic lunginflammation model
Purity 9925Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
BOP sodiumCat No HY-129453
BOP sodium is a potent and selective dual inhibitor with values inα9β1α4β1 integrin Kd
the picomolar range BOP sodium shows the rapidand preferential mobilization of hematopoieticstem cell (HSC) and progenitors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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c(phg-isoDGR-(NMe)k)Cat No HY-111413
c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
c(phg-isoDGR-(NMe)k) TFACat No HY-111413A
c(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
CarotegrastCat No HY-14857
Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor
activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Carotegrast methyl (AJM300) Cat No HY-124290
Carotegrast methyl (AJM300) is an orally activeand selective antagonist HCA2969 anα4 integrinactive metabolite of AJM300 is a specific dualα4β1α4β7 integrin antagonist Carotegrast methylprevents the development of colitis in miceltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cilengitide (EMD 121974) Cat No HY-16141
Cilengitide (EMD 121974) is a potent and selectiveinhibitor of the and integrins α βν 3 α βν 5
Cilengitide inhibits binding of isolated α βν 3
and α β to Vitronectin with an IC value of 4ν 5 50
and 79 nM respectively
Purity 9932Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cilengitide TFA (EMD 121974 TFA) Cat No HY-16143
Cilengitide is a potent and selective integrininhibitor for α β and α β receptor withv 3 v 5
values of 4 nM and 79 nM respectivelyIC50
Purity 9885Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Cucurbitacin BCat No HY-N0416
Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids could represscancer cell progression
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
CWHM-12Cat No HY-18644
CWHM-12 is a potent inhibitor of withαV integrinss of 02 08 15 and 18 nM for IC50 αvβ8
and αvβ3 αvβ6 αvβ1
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK)Cat No HY-P0023
Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin with an of 094 nMα βv 3 IC50
Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK) TFACat No HY-P0023A
Cyclo(-RGDfK) TFA is a potent and selectiveinhibitor of the integrin with an ofα βv 3 IC50
094 nM Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity 9981Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
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Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat No HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof with antitumor activityintegrin αvβ3
Purity 9940Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RADfK)Cat No HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch therapy and diagnosis ofneoangiogenesis
Purity 9803Clinical Data No Development ReportedSize 1 mg
Cyclo(RGDyK)Cat No HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nMintegrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RGDyK) trifluoroacetateCat No HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
E7820 (ER68203-00) Cat No HY-14571
E7820 (ER68203-00) an orally active aromaticsulfonamide derivative is a unique angiogenesisinhibitor suppressing an expression of integrin
subunit on endothelium E7820 inhibits ratalpha2aorta angiogenesis with an of 011 μgmlIC50
Purity 9936Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
EchistatinCat No HY-P1189
Echistatin the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Echistatin TFACat No HY-P1189A
Echistatin TFA the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EptifibatideCat No HY-B0686
Eptifibatide is a cyclic heptapeptide acts as acompetitive antagonist for the activated platelet
with anti-plateletglycoprotein IIbIIIa receptoractivity
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Eptifibatide acetateCat No HY-B0686A
Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Firategrast (SB 683699) Cat No HY-14951
Firategrast (SB 683699) is an orally active andspecific antagonistα4β1α4β7 integrinFirategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) anddecreases multiple sclerosis (MS) activity
Purity 9988Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
wwwMedChemExpresscom 15
ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
wwwMedChemExpresscom 17
SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 21
Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
24 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
wwwMedChemExpresscom 25
BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
wwwMedChemExpresscom 27
DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 35
Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
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Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
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ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
Larazotide acetateCat No HY-106268A
Larazotide acetate is a synthetic peptideLarazotide acetate acts as a tight junctionregulator and reverses leaky junctions to theirnormally closed state
Purity 9968Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Meclofenamate sodium (Meclofenamic acid sodium) Cat No HY-B1320
Meclofenamic acid sodium is a nonsteroidalanti-inflammatory drug (NSAID) approved for use inarthritis (osteo and rheumatoid) analgesia (mildto moderate pain) dysmenorrhea and heavymenstrual blood loss (menorrhagia)
Purity 9862Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 200 mg
Meclofenamic acidCat No HY-117275
Meclofenamic Acid a non-steroidalanti-inflammatory agent is a highly selectivefat mass and obesity-associated (FTO) enzymeinhibitor Meclofenamic Acid competes with FTObinding for the m(6)A-containing nucleic acid
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Rotigaptide (ZP123) Cat No HY-106225
Rotigaptide (ZP123) is a novel and specificmodulator of Rotigaptideconnexin 43 (Cx43)prevents the uncoupling of Cx43-mediated gap
communication and normalizes cell-to-celljunctioncommunication during acute metabolic stress
Purity 9963Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg
TAT-Gap19Cat No HY-P1136B
TAT-Gap19 a Cx mimetic peptide is a specific inhibitorconnexin43 hemichannel (Cx43 HC)
TAT-Gap19 does not inhibits the corresponding Cx43GJCs TAT-Gap19 traverses the blood-brain barrierand alleviate liver fibrosis in mice
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tonabersat (SB-220453) Cat No HY-15204
Tonabersat (SB-220453) is a modulatorgap-junctionTonabersat prevents inflammatory damage in thecentral nervous system
Purity 9968Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
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Integrin
Integrins a family of heterodimeric adhesion receptors for diverse extracellular matrices have consistently been implicated ascrucial drivers of ovarian cancer development and progression A number of the RGD-based members of the integrin familyincluding α5β1 and αvβ3 or αvβ5 integrins are markedly elevated in aggressive ovarian tumors These adhesion receptors appearto promote cell adhesion survival motility and invasion during ovarian tumor growth or metastatic progression Importantly thefunctions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signalingincluding the PI3KAkt- and RasMAPK-dependent pathways
Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion Modulationof these molecules particularly αv integrin family has exhibited profound effects on fibrosis in multiple organ and disease stateBased on the several studies the integrins αvβ3 αvβ5 αvβ6 and αvβ8 have been known to modulate the fibrotic process viaactivation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis
Each integrin is typically formed by the non-covalent pairing of one α subunit of which 18 types are known to exist and one βsubunit of which 8 types are known to exist Together 24 distinct heterodimers have been identified to date The αv subunit canform heterodimers with the β1 β3 β5 β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11 andαv indicating that not all theoretically possible α and subunit pairs form Interestingly the activation of TGF-β appears to be acommon function of multiple αv integrins
wwwMedChemExpresscom 11
Integrin Inhibitors Agonists Antagonists amp Modulators
A-205804Cat No HY-100226
A-205804 is an orally bioavailable potent andselective lead inhibitor of andE-selectin
expression with an of 20 nM and 25ICAM-1 IC50
nM for E-selectin and ICAM-1 respectivelyA-205804 can be used in the research of chronicinflammatory diseases
Purity 9812Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Arg-Gly-Asp-Ser (RGDS peptide Fibronectin tetrapeptide) Cat No HY-12290
Arg-Gly-Asp-Ser is an integrin binding sequencethat inhibits functionintegrin receptordecreases systemic inflammation via inhibition ofcollagen-triggered activation of leukocytes andattenuates expression of inflammatory cytokinesiNOS and MMP-9
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Arg-Gly-Asp-Ser (TFA) (RGDS peptide (TFA) Fibronectin tetrapeptide (TFA)) Cat No HY-12290A
Arg-Gly-Asp-Ser (TFA) is an integrin bindingsequence that inhibits functionintegrin receptorArg-Gly-Asp-Ser (TFA) directly and specificallybind pro-caspase-8 pro-caspase-9 andpro-caspase-3 while it does not bindpro-caspase-1
Purity gt98Clinical DataSize 1 mg 5 mg
ATN-161 trifluoroacetate salt (ATN-161 TFA salt) Cat No HY-13535A
ATN-161 trifluoroacetate salt is a novel integrin antagonist which inhibits angiogenesis andα5β1
growth of liver metastases in a murine model
Purity ge950Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg
BI-1950Cat No HY-124040
BI-1950 is a highly potent lymphocyte function inhibitor LFA-1 isassociated antigen-1 (LFA-1)
an essential component in normal immune systemfunction and a target for drug discovery
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO-1211Cat No HY-14126
BIO-1211 is a highly selective and orally active inhibitor with values of 4 nMα4β1 (VLA-4) IC50
and 2 μM for α4β1 and α4β7 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192Cat No HY-107589
BIO5192 is a selective and potent integrin α4β1(VLA-4) inhibitor ( lt10 pM) BIO5192Kd
selectively binds to α4β1 ( =18 nM) over aIC50
range of other integrins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192 hydrateCat No HY-107589A
BIO5192 hydrate is a selective and potent integrin inhibitor ( lt10 pM) BIO5192α4β1 (VLA-4) Kd
hydrate selectively binds to α4β1 ( =18 nM)IC50
over a range of other integrins
Purity ge980Clinical Data No Development ReportedSize 1 mg
BMS-688521Cat No HY-10596
BMS-688521 is a highly potent orally activeinhibitor of the interaction withLFA-1ICAMan of 25 nM in the adhesion assay and anIC50
of 60 nM in the MLR assay BMS-688521 isIC50
efficacious in a mouse allergic eosinophilic lunginflammation model
Purity 9925Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
BOP sodiumCat No HY-129453
BOP sodium is a potent and selective dual inhibitor with values inα9β1α4β1 integrin Kd
the picomolar range BOP sodium shows the rapidand preferential mobilization of hematopoieticstem cell (HSC) and progenitors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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c(phg-isoDGR-(NMe)k)Cat No HY-111413
c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
c(phg-isoDGR-(NMe)k) TFACat No HY-111413A
c(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
CarotegrastCat No HY-14857
Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor
activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Carotegrast methyl (AJM300) Cat No HY-124290
Carotegrast methyl (AJM300) is an orally activeand selective antagonist HCA2969 anα4 integrinactive metabolite of AJM300 is a specific dualα4β1α4β7 integrin antagonist Carotegrast methylprevents the development of colitis in miceltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cilengitide (EMD 121974) Cat No HY-16141
Cilengitide (EMD 121974) is a potent and selectiveinhibitor of the and integrins α βν 3 α βν 5
Cilengitide inhibits binding of isolated α βν 3
and α β to Vitronectin with an IC value of 4ν 5 50
and 79 nM respectively
Purity 9932Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cilengitide TFA (EMD 121974 TFA) Cat No HY-16143
Cilengitide is a potent and selective integrininhibitor for α β and α β receptor withv 3 v 5
values of 4 nM and 79 nM respectivelyIC50
Purity 9885Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Cucurbitacin BCat No HY-N0416
Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids could represscancer cell progression
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
CWHM-12Cat No HY-18644
CWHM-12 is a potent inhibitor of withαV integrinss of 02 08 15 and 18 nM for IC50 αvβ8
and αvβ3 αvβ6 αvβ1
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK)Cat No HY-P0023
Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin with an of 094 nMα βv 3 IC50
Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK) TFACat No HY-P0023A
Cyclo(-RGDfK) TFA is a potent and selectiveinhibitor of the integrin with an ofα βv 3 IC50
094 nM Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity 9981Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
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Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat No HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof with antitumor activityintegrin αvβ3
Purity 9940Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RADfK)Cat No HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch therapy and diagnosis ofneoangiogenesis
Purity 9803Clinical Data No Development ReportedSize 1 mg
Cyclo(RGDyK)Cat No HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nMintegrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RGDyK) trifluoroacetateCat No HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
E7820 (ER68203-00) Cat No HY-14571
E7820 (ER68203-00) an orally active aromaticsulfonamide derivative is a unique angiogenesisinhibitor suppressing an expression of integrin
subunit on endothelium E7820 inhibits ratalpha2aorta angiogenesis with an of 011 μgmlIC50
Purity 9936Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
EchistatinCat No HY-P1189
Echistatin the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Echistatin TFACat No HY-P1189A
Echistatin TFA the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EptifibatideCat No HY-B0686
Eptifibatide is a cyclic heptapeptide acts as acompetitive antagonist for the activated platelet
with anti-plateletglycoprotein IIbIIIa receptoractivity
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Eptifibatide acetateCat No HY-B0686A
Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Firategrast (SB 683699) Cat No HY-14951
Firategrast (SB 683699) is an orally active andspecific antagonistα4β1α4β7 integrinFirategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) anddecreases multiple sclerosis (MS) activity
Purity 9988Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
wwwMedChemExpresscom 15
ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
wwwMedChemExpresscom 17
SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 19
Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 21
Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
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AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
wwwMedChemExpresscom 25
BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
wwwMedChemExpresscom 27
DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 35
Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
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Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 51
ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
Integrin
Integrins a family of heterodimeric adhesion receptors for diverse extracellular matrices have consistently been implicated ascrucial drivers of ovarian cancer development and progression A number of the RGD-based members of the integrin familyincluding α5β1 and αvβ3 or αvβ5 integrins are markedly elevated in aggressive ovarian tumors These adhesion receptors appearto promote cell adhesion survival motility and invasion during ovarian tumor growth or metastatic progression Importantly thefunctions of these integrins are strongly dependent on the activation of focal adhesion kinase (FAK) and its downstream signalingincluding the PI3KAkt- and RasMAPK-dependent pathways
Integrins are transmembrane proteins and are major receptors for cell-extracellular matrix (ECM) and cell-cell adhesion Modulationof these molecules particularly αv integrin family has exhibited profound effects on fibrosis in multiple organ and disease stateBased on the several studies the integrins αvβ3 αvβ5 αvβ6 and αvβ8 have been known to modulate the fibrotic process viaactivation of latent transforming growth factor (TGF)-β in pre-clinical models of fibrosis
Each integrin is typically formed by the non-covalent pairing of one α subunit of which 18 types are known to exist and one βsubunit of which 8 types are known to exist Together 24 distinct heterodimers have been identified to date The αv subunit canform heterodimers with the β1 β3 β5 β6 or β8 subunits and β1 can associate with many different α subunits from α1 to α11 andαv indicating that not all theoretically possible α and subunit pairs form Interestingly the activation of TGF-β appears to be acommon function of multiple αv integrins
wwwMedChemExpresscom 11
Integrin Inhibitors Agonists Antagonists amp Modulators
A-205804Cat No HY-100226
A-205804 is an orally bioavailable potent andselective lead inhibitor of andE-selectin
expression with an of 20 nM and 25ICAM-1 IC50
nM for E-selectin and ICAM-1 respectivelyA-205804 can be used in the research of chronicinflammatory diseases
Purity 9812Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Arg-Gly-Asp-Ser (RGDS peptide Fibronectin tetrapeptide) Cat No HY-12290
Arg-Gly-Asp-Ser is an integrin binding sequencethat inhibits functionintegrin receptordecreases systemic inflammation via inhibition ofcollagen-triggered activation of leukocytes andattenuates expression of inflammatory cytokinesiNOS and MMP-9
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Arg-Gly-Asp-Ser (TFA) (RGDS peptide (TFA) Fibronectin tetrapeptide (TFA)) Cat No HY-12290A
Arg-Gly-Asp-Ser (TFA) is an integrin bindingsequence that inhibits functionintegrin receptorArg-Gly-Asp-Ser (TFA) directly and specificallybind pro-caspase-8 pro-caspase-9 andpro-caspase-3 while it does not bindpro-caspase-1
Purity gt98Clinical DataSize 1 mg 5 mg
ATN-161 trifluoroacetate salt (ATN-161 TFA salt) Cat No HY-13535A
ATN-161 trifluoroacetate salt is a novel integrin antagonist which inhibits angiogenesis andα5β1
growth of liver metastases in a murine model
Purity ge950Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg
BI-1950Cat No HY-124040
BI-1950 is a highly potent lymphocyte function inhibitor LFA-1 isassociated antigen-1 (LFA-1)
an essential component in normal immune systemfunction and a target for drug discovery
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO-1211Cat No HY-14126
BIO-1211 is a highly selective and orally active inhibitor with values of 4 nMα4β1 (VLA-4) IC50
and 2 μM for α4β1 and α4β7 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192Cat No HY-107589
BIO5192 is a selective and potent integrin α4β1(VLA-4) inhibitor ( lt10 pM) BIO5192Kd
selectively binds to α4β1 ( =18 nM) over aIC50
range of other integrins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192 hydrateCat No HY-107589A
BIO5192 hydrate is a selective and potent integrin inhibitor ( lt10 pM) BIO5192α4β1 (VLA-4) Kd
hydrate selectively binds to α4β1 ( =18 nM)IC50
over a range of other integrins
Purity ge980Clinical Data No Development ReportedSize 1 mg
BMS-688521Cat No HY-10596
BMS-688521 is a highly potent orally activeinhibitor of the interaction withLFA-1ICAMan of 25 nM in the adhesion assay and anIC50
of 60 nM in the MLR assay BMS-688521 isIC50
efficacious in a mouse allergic eosinophilic lunginflammation model
Purity 9925Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
BOP sodiumCat No HY-129453
BOP sodium is a potent and selective dual inhibitor with values inα9β1α4β1 integrin Kd
the picomolar range BOP sodium shows the rapidand preferential mobilization of hematopoieticstem cell (HSC) and progenitors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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c(phg-isoDGR-(NMe)k)Cat No HY-111413
c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
c(phg-isoDGR-(NMe)k) TFACat No HY-111413A
c(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
CarotegrastCat No HY-14857
Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor
activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Carotegrast methyl (AJM300) Cat No HY-124290
Carotegrast methyl (AJM300) is an orally activeand selective antagonist HCA2969 anα4 integrinactive metabolite of AJM300 is a specific dualα4β1α4β7 integrin antagonist Carotegrast methylprevents the development of colitis in miceltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cilengitide (EMD 121974) Cat No HY-16141
Cilengitide (EMD 121974) is a potent and selectiveinhibitor of the and integrins α βν 3 α βν 5
Cilengitide inhibits binding of isolated α βν 3
and α β to Vitronectin with an IC value of 4ν 5 50
and 79 nM respectively
Purity 9932Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cilengitide TFA (EMD 121974 TFA) Cat No HY-16143
Cilengitide is a potent and selective integrininhibitor for α β and α β receptor withv 3 v 5
values of 4 nM and 79 nM respectivelyIC50
Purity 9885Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Cucurbitacin BCat No HY-N0416
Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids could represscancer cell progression
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
CWHM-12Cat No HY-18644
CWHM-12 is a potent inhibitor of withαV integrinss of 02 08 15 and 18 nM for IC50 αvβ8
and αvβ3 αvβ6 αvβ1
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK)Cat No HY-P0023
Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin with an of 094 nMα βv 3 IC50
Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK) TFACat No HY-P0023A
Cyclo(-RGDfK) TFA is a potent and selectiveinhibitor of the integrin with an ofα βv 3 IC50
094 nM Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity 9981Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
wwwMedChemExpresscom 13
Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat No HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof with antitumor activityintegrin αvβ3
Purity 9940Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RADfK)Cat No HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch therapy and diagnosis ofneoangiogenesis
Purity 9803Clinical Data No Development ReportedSize 1 mg
Cyclo(RGDyK)Cat No HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nMintegrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RGDyK) trifluoroacetateCat No HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
E7820 (ER68203-00) Cat No HY-14571
E7820 (ER68203-00) an orally active aromaticsulfonamide derivative is a unique angiogenesisinhibitor suppressing an expression of integrin
subunit on endothelium E7820 inhibits ratalpha2aorta angiogenesis with an of 011 μgmlIC50
Purity 9936Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
EchistatinCat No HY-P1189
Echistatin the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Echistatin TFACat No HY-P1189A
Echistatin TFA the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EptifibatideCat No HY-B0686
Eptifibatide is a cyclic heptapeptide acts as acompetitive antagonist for the activated platelet
with anti-plateletglycoprotein IIbIIIa receptoractivity
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Eptifibatide acetateCat No HY-B0686A
Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Firategrast (SB 683699) Cat No HY-14951
Firategrast (SB 683699) is an orally active andspecific antagonistα4β1α4β7 integrinFirategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) anddecreases multiple sclerosis (MS) activity
Purity 9988Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
wwwMedChemExpresscom 15
ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
wwwMedChemExpresscom 17
SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 19
Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 21
Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
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AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
wwwMedChemExpresscom 25
BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
wwwMedChemExpresscom 27
DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
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Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
50 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 51
ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
52 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
Integrin Inhibitors Agonists Antagonists amp Modulators
A-205804Cat No HY-100226
A-205804 is an orally bioavailable potent andselective lead inhibitor of andE-selectin
expression with an of 20 nM and 25ICAM-1 IC50
nM for E-selectin and ICAM-1 respectivelyA-205804 can be used in the research of chronicinflammatory diseases
Purity 9812Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Arg-Gly-Asp-Ser (RGDS peptide Fibronectin tetrapeptide) Cat No HY-12290
Arg-Gly-Asp-Ser is an integrin binding sequencethat inhibits functionintegrin receptordecreases systemic inflammation via inhibition ofcollagen-triggered activation of leukocytes andattenuates expression of inflammatory cytokinesiNOS and MMP-9
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Arg-Gly-Asp-Ser (TFA) (RGDS peptide (TFA) Fibronectin tetrapeptide (TFA)) Cat No HY-12290A
Arg-Gly-Asp-Ser (TFA) is an integrin bindingsequence that inhibits functionintegrin receptorArg-Gly-Asp-Ser (TFA) directly and specificallybind pro-caspase-8 pro-caspase-9 andpro-caspase-3 while it does not bindpro-caspase-1
Purity gt98Clinical DataSize 1 mg 5 mg
ATN-161 trifluoroacetate salt (ATN-161 TFA salt) Cat No HY-13535A
ATN-161 trifluoroacetate salt is a novel integrin antagonist which inhibits angiogenesis andα5β1
growth of liver metastases in a murine model
Purity ge950Clinical Data Phase 2Size 5 mg 10 mg 50 mg 100 mg
BI-1950Cat No HY-124040
BI-1950 is a highly potent lymphocyte function inhibitor LFA-1 isassociated antigen-1 (LFA-1)
an essential component in normal immune systemfunction and a target for drug discovery
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO-1211Cat No HY-14126
BIO-1211 is a highly selective and orally active inhibitor with values of 4 nMα4β1 (VLA-4) IC50
and 2 μM for α4β1 and α4β7 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192Cat No HY-107589
BIO5192 is a selective and potent integrin α4β1(VLA-4) inhibitor ( lt10 pM) BIO5192Kd
selectively binds to α4β1 ( =18 nM) over aIC50
range of other integrins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BIO5192 hydrateCat No HY-107589A
BIO5192 hydrate is a selective and potent integrin inhibitor ( lt10 pM) BIO5192α4β1 (VLA-4) Kd
hydrate selectively binds to α4β1 ( =18 nM)IC50
over a range of other integrins
Purity ge980Clinical Data No Development ReportedSize 1 mg
BMS-688521Cat No HY-10596
BMS-688521 is a highly potent orally activeinhibitor of the interaction withLFA-1ICAMan of 25 nM in the adhesion assay and anIC50
of 60 nM in the MLR assay BMS-688521 isIC50
efficacious in a mouse allergic eosinophilic lunginflammation model
Purity 9925Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
BOP sodiumCat No HY-129453
BOP sodium is a potent and selective dual inhibitor with values inα9β1α4β1 integrin Kd
the picomolar range BOP sodium shows the rapidand preferential mobilization of hematopoieticstem cell (HSC) and progenitors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
12 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
c(phg-isoDGR-(NMe)k)Cat No HY-111413
c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
c(phg-isoDGR-(NMe)k) TFACat No HY-111413A
c(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
CarotegrastCat No HY-14857
Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor
activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Carotegrast methyl (AJM300) Cat No HY-124290
Carotegrast methyl (AJM300) is an orally activeand selective antagonist HCA2969 anα4 integrinactive metabolite of AJM300 is a specific dualα4β1α4β7 integrin antagonist Carotegrast methylprevents the development of colitis in miceltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cilengitide (EMD 121974) Cat No HY-16141
Cilengitide (EMD 121974) is a potent and selectiveinhibitor of the and integrins α βν 3 α βν 5
Cilengitide inhibits binding of isolated α βν 3
and α β to Vitronectin with an IC value of 4ν 5 50
and 79 nM respectively
Purity 9932Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cilengitide TFA (EMD 121974 TFA) Cat No HY-16143
Cilengitide is a potent and selective integrininhibitor for α β and α β receptor withv 3 v 5
values of 4 nM and 79 nM respectivelyIC50
Purity 9885Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Cucurbitacin BCat No HY-N0416
Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids could represscancer cell progression
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
CWHM-12Cat No HY-18644
CWHM-12 is a potent inhibitor of withαV integrinss of 02 08 15 and 18 nM for IC50 αvβ8
and αvβ3 αvβ6 αvβ1
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK)Cat No HY-P0023
Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin with an of 094 nMα βv 3 IC50
Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK) TFACat No HY-P0023A
Cyclo(-RGDfK) TFA is a potent and selectiveinhibitor of the integrin with an ofα βv 3 IC50
094 nM Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity 9981Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
wwwMedChemExpresscom 13
Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat No HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof with antitumor activityintegrin αvβ3
Purity 9940Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RADfK)Cat No HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch therapy and diagnosis ofneoangiogenesis
Purity 9803Clinical Data No Development ReportedSize 1 mg
Cyclo(RGDyK)Cat No HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nMintegrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RGDyK) trifluoroacetateCat No HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
E7820 (ER68203-00) Cat No HY-14571
E7820 (ER68203-00) an orally active aromaticsulfonamide derivative is a unique angiogenesisinhibitor suppressing an expression of integrin
subunit on endothelium E7820 inhibits ratalpha2aorta angiogenesis with an of 011 μgmlIC50
Purity 9936Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
EchistatinCat No HY-P1189
Echistatin the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Echistatin TFACat No HY-P1189A
Echistatin TFA the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EptifibatideCat No HY-B0686
Eptifibatide is a cyclic heptapeptide acts as acompetitive antagonist for the activated platelet
with anti-plateletglycoprotein IIbIIIa receptoractivity
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Eptifibatide acetateCat No HY-B0686A
Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Firategrast (SB 683699) Cat No HY-14951
Firategrast (SB 683699) is an orally active andspecific antagonistα4β1α4β7 integrinFirategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) anddecreases multiple sclerosis (MS) activity
Purity 9988Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
14 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
wwwMedChemExpresscom 15
ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
16 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
wwwMedChemExpresscom 17
SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 19
Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 21
Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
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AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
wwwMedChemExpresscom 25
BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
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Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
wwwMedChemExpresscom 27
DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 35
Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
36 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 51
ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
c(phg-isoDGR-(NMe)k)Cat No HY-111413
c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
c(phg-isoDGR-(NMe)k) TFACat No HY-111413A
c(phg-isoDGR-(NMe)k) TFA is a selective and potent ligand with an of 29 nMα5β1-integrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
CarotegrastCat No HY-14857
Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor
activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Carotegrast methyl (AJM300) Cat No HY-124290
Carotegrast methyl (AJM300) is an orally activeand selective antagonist HCA2969 anα4 integrinactive metabolite of AJM300 is a specific dualα4β1α4β7 integrin antagonist Carotegrast methylprevents the development of colitis in miceltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cilengitide (EMD 121974) Cat No HY-16141
Cilengitide (EMD 121974) is a potent and selectiveinhibitor of the and integrins α βν 3 α βν 5
Cilengitide inhibits binding of isolated α βν 3
and α β to Vitronectin with an IC value of 4ν 5 50
and 79 nM respectively
Purity 9932Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cilengitide TFA (EMD 121974 TFA) Cat No HY-16143
Cilengitide is a potent and selective integrininhibitor for α β and α β receptor withv 3 v 5
values of 4 nM and 79 nM respectivelyIC50
Purity 9885Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Cucurbitacin BCat No HY-N0416
Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids could represscancer cell progression
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
CWHM-12Cat No HY-18644
CWHM-12 is a potent inhibitor of withαV integrinss of 02 08 15 and 18 nM for IC50 αvβ8
and αvβ3 αvβ6 αvβ1
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK)Cat No HY-P0023
Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin with an of 094 nMα βv 3 IC50
Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cyclo(-RGDfK) TFACat No HY-P0023A
Cyclo(-RGDfK) TFA is a potent and selectiveinhibitor of the integrin with an ofα βv 3 IC50
094 nM Cyclo(-RGDfK) TFA potently targets tumormicrovasculature and cancer cells through thespecific binding to the αvβ3 integrin on the cellsurface
Purity 9981Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
wwwMedChemExpresscom 13
Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat No HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof with antitumor activityintegrin αvβ3
Purity 9940Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RADfK)Cat No HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch therapy and diagnosis ofneoangiogenesis
Purity 9803Clinical Data No Development ReportedSize 1 mg
Cyclo(RGDyK)Cat No HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nMintegrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RGDyK) trifluoroacetateCat No HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
E7820 (ER68203-00) Cat No HY-14571
E7820 (ER68203-00) an orally active aromaticsulfonamide derivative is a unique angiogenesisinhibitor suppressing an expression of integrin
subunit on endothelium E7820 inhibits ratalpha2aorta angiogenesis with an of 011 μgmlIC50
Purity 9936Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
EchistatinCat No HY-P1189
Echistatin the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Echistatin TFACat No HY-P1189A
Echistatin TFA the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EptifibatideCat No HY-B0686
Eptifibatide is a cyclic heptapeptide acts as acompetitive antagonist for the activated platelet
with anti-plateletglycoprotein IIbIIIa receptoractivity
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Eptifibatide acetateCat No HY-B0686A
Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Firategrast (SB 683699) Cat No HY-14951
Firategrast (SB 683699) is an orally active andspecific antagonistα4β1α4β7 integrinFirategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) anddecreases multiple sclerosis (MS) activity
Purity 9988Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
wwwMedChemExpresscom 15
ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
wwwMedChemExpresscom 17
SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 19
Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 21
Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
24 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
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BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
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DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 35
Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
36 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
42 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 51
ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat No HY-P1613A
Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof with antitumor activityintegrin αvβ3
Purity 9940Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RADfK)Cat No HY-P0031
Cyclo(RADfK) is a selective α(v)β(3) integrinligand that has been extensively used forresearch therapy and diagnosis ofneoangiogenesis
Purity 9803Clinical Data No Development ReportedSize 1 mg
Cyclo(RGDyK)Cat No HY-100563A
Cyclo(RGDyK) is a potent and selective α βV 3
inhibitor with an of 20 nMintegrin IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cyclo(RGDyK) trifluoroacetateCat No HY-100563
Cyclo(RGDyK) trifluoroacetate is a potent andselective inhibitor with an α β integrinV 3 IC50
of 20 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
E7820 (ER68203-00) Cat No HY-14571
E7820 (ER68203-00) an orally active aromaticsulfonamide derivative is a unique angiogenesisinhibitor suppressing an expression of integrin
subunit on endothelium E7820 inhibits ratalpha2aorta angiogenesis with an of 011 μgmlIC50
Purity 9936Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
EchistatinCat No HY-P1189
Echistatin the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Echistatin TFACat No HY-P1189A
Echistatin TFA the smallest active RGD proteinbelonging to the family of disintegrins that arederived from snake venoms is a potent inhibitorof Echistatin is a potentplatelet aggregationinhibitor of in culturebone resorption
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EptifibatideCat No HY-B0686
Eptifibatide is a cyclic heptapeptide acts as acompetitive antagonist for the activated platelet
with anti-plateletglycoprotein IIbIIIa receptoractivity
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Eptifibatide acetateCat No HY-B0686A
Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Firategrast (SB 683699) Cat No HY-14951
Firategrast (SB 683699) is an orally active andspecific antagonistα4β1α4β7 integrinFirategrast reduces trafficking of lymphocytesinto the central nervous system (CNS) anddecreases multiple sclerosis (MS) activity
Purity 9988Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
wwwMedChemExpresscom 15
ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
wwwMedChemExpresscom 17
SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 19
Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 21
Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
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AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
wwwMedChemExpresscom 25
BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
wwwMedChemExpresscom 27
DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 35
Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
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Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 51
ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
Fradafiban (BIBU-52) Cat No HY-101720
Fradafiban is a nonpeptide platelet glycoproteinIIbIIIa antagonist which binds to the humanplatelet GP IIbIIIa complex with a K value ofd
148 nM
Purity gt98Clinical Data Phase 1Size 1 mg 5 mg
GLPG0187Cat No HY-100506
GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50
Purity 9897Clinical Data Phase 1Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
Gly-Arg-Gly-Asp-SerCat No HY-P0295
Gly-Arg-Gly-Asp-Ser is a pentapeptide that formsthe cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50
and 65 μM
Purity 9505Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg 25 mg
Gly-Arg-Gly-Asp-Ser (TFA)Cat No HY-P0295A
Gly-Arg-Gly-Asp-Ser (TFA) is a pentapeptide thatforms the cell-binding domain of a glycoproteinosteopontin Gly-Arg-Gly-Asp-Ser binds to integrin
αvβ3 and αvβ5 with estimated of 5receptors IC50
and 65 μM
Purity gt98Clinical DataSize 1 mg 5 mg
GRGDSPCat No HY-P0290
GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
GRGDSP TFACat No HY-P0290A
GRGDSP (TFA) is an inhibitorintegrin
Purity 9853Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
HSDVHK-NH2Cat No HY-P1187
HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity 9963Clinical Data No Development ReportedSize 5 mg 10 mg
HSDVHK-NH2 TFACat No HY-P1187A
HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50
pgmL (2414 pM)ltbrgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ICAM-1-IN-1Cat No HY-U00003
ICAM-1-IN-1 is a potent and selective inhibitor of and with values of 7 andE-selectin ICAM-1 IC50
5 nM respectively
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
ILK-IN-2 (OSU-T315 analog) Cat No HY-18676B
ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg
wwwMedChemExpresscom 15
ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
wwwMedChemExpresscom 17
SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 19
Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 21
Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
24 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
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BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
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DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 35
Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
36 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 51
ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
ILK-IN-3Cat No HY-115677
ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity
Purity 9957Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin Antagonists 27Cat No HY-18668
Integrin Antagonists 27 is a small moleculeintegrin αvβ3 antagonist with binding affinity of18 nM as s novel anticancer agent
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Integrin modulator 1Cat No HY-134130
Integrin modulator 1 is a potent and selective agonist with an of 98 nM forα4β1 integrin IC50
RGD-binding α4β1 Integrin modulator 1 increasescell adhesion mediated by α4β1 integrin with an
of 129 nMEC50
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Integrin-IN-2Cat No HY-130119
Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitorαv integrinIntegrin-IN-2 can increases the αvβ6 αvβ3
and binding affinities with αvβ5 αvβ8 pIC50
values of 78 84 84 and 74 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
iRGD peptide (c(CRGDKGPDC)) Cat No HY-P0122
iRGD peptide is a 9-amino acid cyclic peptidetriggers tissue penetration of drugs by firstbinding to then proteolyticallyav integrinscleaved in the tumor to produce CRGDKR tointeract with neuropilin-1 and hastumor-targeting and tumor-penetrating properties
Purity 9903Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
IrigeninCat No HY-N2587
Irigenin is a is a lead compound and mediates itsanti-metastatic effect by specifically andselectively blocking and integrinsα9β1 α4β1binding sites on C-C loop of Extra Domain A (EDA)Irigenin shows anti-cancer properties
Purity 9984Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
LDVCat No HY-P2267
LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Leukadherin-1Cat No HY-15701
Leukadherin-1 a specific agonist of the leukocytesurface integrin increasesCD11bCD18CD11bCD18-dependent cell adhesion to fibrinogenwith an EC of 4 μM50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Lifitegrast (SAR 1118 SHP-606) Cat No HY-19344
Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonistLFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 298 nMIC50
Purity 9958Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
LXW7Cat No HY-P0178
LXW7 a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 increases phosphorylation ofIC50
VEGFR-2 and activation of ERK12Anti-inflammatory effect
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
wwwMedChemExpresscom 17
SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 19
Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 21
Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
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AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
wwwMedChemExpresscom 25
BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
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Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
wwwMedChemExpresscom 27
DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 35
Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
36 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
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HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 51
ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
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Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 53
LXW7 TFACat No HY-P0178A
LXW7 TFA a cyclic peptide containing Arg-Gly-Asp(RGD) is an inhibitor LXW7 has aintegrin αvβ3high binding affinity to with anαvβ3 integrin
of 068 μM LXW7 TFA increasesIC50
phosphorylation of VEGFR-2 and activation ofERK12 Anti-inflammatory effect
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
MK-0429 (L-000845704) Cat No HY-15102
MK-0429 (L-000845704) is an orally active potentselective and nonpeptide antagonistpan-integrinwith values of 16 nM 28 nM 01 nM 07IC50
nM 05 nM and 122 nM for αvβ1 αvβ3 αvβ5 αvβ6αvβ8 and α5β1 respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
NatalizumabCat No HY-108831
Natalizumab is a recombinant humanized monoclonalantibody binds to α4β1- and blocks itsintegrininteraction with vascular cell adhesion molecule-1(VCAM-1) Natalizumab can be used for thetreatment of relapsing remitting multiplesclerosis and Crohns disease
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg 10 mg
OSU-T315Cat No HY-18676
OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 06 μM(ILK) 50
inhibiting PI3KAKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain)
Purity 9988Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
PyrintegrinCat No HY-13306
Pyrintegrin is an agonist and aβ1-integrin24-disubstituted pyrimidine that promotesembryonic stem cells survival Pyrintegrinenhances cell-extracellular matrix (ECM)adhesion-mediated signalingintegrin
Purity 9704Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
RGDCat No HY-P0278
RGD is a tripeptide that effectively triggers celladhesion addresses certain cell lines and elicitsspecific cell responses binds to integrins
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
RGD peptide (GRGDNP)Cat No HY-P1740
RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
RGD peptide (GRGDNP) (TFA)Cat No HY-P1740A
RGD peptide (GRGDNP) (TFA) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion migrationgrowth and differentiation
Purity 9880Clinical Data No Development ReportedSize 1 mg 5 mg
RGD TrifluoroacetateCat No HY-P0278A
RGD Trifluoroacetate is a tripeptide thateffectively triggers cell adhesion addressescertain cell lines and elicits specific cellresponses RGD Trifluoroacetate binds to integrins
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
RWJ 50271Cat No HY-110086
RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1intercellular adhesion
interaction with anmolecule-1(LFA-1ICAM-1) of 50 μM (HL60 cells) RWJ 50271 inhibitsIC50
LFA-1ICAM-1-mediated cell adhesion
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
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SB-267268Cat No HY-19306
SB-267268 is a selective and nonpeptidic and alpha(v)beta3 (αvβ3) alpha(v)beta5 (αvβ5)
integrins antagonist with s of 09 05 and 07Ki
nM for human αvβ3 monkey αvβ3 and human αvβ5respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Sibrafiban (RO 48-3657) Cat No HY-10309
Sibrafiban (RO 48-3657) is the orally activenonpeptide double-prodrug of Ro 44-3888 and aselective glycoprotein IIbIIIa receptorantagonist Sibrafiban inhibits plateletaggregation
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SR121566ACat No HY-U00235
SR121566A is a novel non-peptide Glycoprotein ( ) antagonist which canIIbIIIa GP IIb-IIIa
inhibit ADP- arachidonic acid- andcollagen-induced human platelet aggregation with
s of 46plusmn75 56plusmn6 and 42plusmn3 nM respectivelyIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TCS 2314Cat No HY-12308
TCS 2314 (compound 3) is orally active andselective very late antigen-4 (VLA-4 α4β1
antagonist with an of 44 nMCD49dCD29) IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg
Tetrac (Tetraiodothyroacetic acid
3355-Tetraiodothyroacetic acid) Cat No HY-W008859
Tetrac (Tetraiodothyroacetic acid) a derivativeof L-thyroxine (T4) is a thyrointegrin receptorantagonist Tetrac blocks the actions of T4 and353-triiodo-L-thyronine (T3) at the cellsurface receptor for thyroid hormone on integrin
αvβ3
Purity ge950Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg
THI0019Cat No HY-117388
THI0019 is a potent agonistintegrin α4β1 (VLA-4)with an range of 1-2 μM THI0019 inducesEC50
stemprogenitor cells adhesion THI0019 alsoregulates adhesion mediated by α4β7 α5β1 andαLβ2
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg
Tirofiban (L700462 MK383) Cat No HY-17369B
Tirofiban(L700462MK383) is a potent non-peptideglycoprotein IIbIIIa (integrins alphaIIbbetaIII)antagonist Target integrin IIbIIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Tirofiban hydrochloride monohydrateCat No HY-17369
Tirofiban hydrochloride monohydrate is a potentnon-peptide glycoprotein IIbIIIa (integrinsalphaIIbbetaIII) antagonist IC50 value Targetintegrin IIbIIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation
Purity 9934Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
TR-14035Cat No HY-15770
TR-14035 is a dual α β α integrin4 7 4 1β
antagonist with s of 7 nM and 87 nM forIC50
α β and α respectively TR-14035 can be4 7 4 1β
used for the research of inflammation andautoimmune disease
Purity 9514Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valategrast (R-411 free base) Cat No HY-14190
Valategrast (R-411 free base) is a potent andorally active and dualintegrin α4β1 (VLA-4) α4β7antagonist Valategrast has the potential forChronic obstructive pulmonary disease (COPD) andasthma treatment
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Vedolizumab (Anti-Human lymphocyte α4β7 integrin Humanized Antibody) Cat No HY-P9911
Vedolizumab is a humanized monoclonal antibodythat targets the α4β7 for the treatment ofintegrinulcerative colitis and Crohns disease
Purity 9964Clinical Data LaunchedSize 1 mg 5 mg 25 mg 50 mg
Zaurategrast (CT7758) Cat No HY-70073
Zaurategrast (CT7758) is a potent andoral-effective inhibitorα -integrin4
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
Zaurategrast ethyl ester (CDP323 UCB1184197) Cat No HY-75385
Zaurategrast ethyl ester (CDP323) the ethyl esterprodrug of CT7758 is a integrinα4β1 α4β7antagonist used for the treatment of inflammatoryand autoimmune disorders
Purity 9906Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
Zaurategrast ethyl ester sulfate (CDP323 sulfate UCB1184197 sulfate) Cat No HY-75385A
Zaurategrast ethyl ester sulfate (CDP323 sulfate)the ethyl ester prodrug of CT7758 is a
integrin antagonist used for theα4β1 α4β7treatment of inflammatory and autoimmunedisorders
Purity gt98Clinical Data Phase 2Size 1 mg 5 mg
α2β1 Integrin Ligand PeptideCat No HY-P1868
α2β1 Integrin Ligand Peptide interacts with theα2β1 integrin receptor on the cell membrane andmediates extracellular signals into cells It is apotential antagonist of collagen receptors
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
α2β1 Integrin Ligand Peptide TFACat No HY-P1868A
α2β1 Integrin Ligand Peptide TFA interacts withthe α2β1 integrin receptor on the cell membraneand mediates extracellular signals into cells Itis a potential antagonist of collagen receptors
Purity 9933Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
αvβ1 integrin-IN-1Cat No HY-100445
αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50
063 nM Antifibrotic effects
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
αvβ1 integrin-IN-1 TFACat No HY-100445A
αvβ1 integrin-IN-1 TFA (Compound C8) is a potentand selective inhibitor with an αvβ1 integrin IC50
of 063 nM Antifibrotic effects
Purity 9830Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 19
Kinesin
Kinesins are a family of molecular motors that use the energy of ATP hydrolysis to move along the surface of or destabilizemicrotubule filaments The kinesin motor protein family consists of 14 distinct subclasses and 45 kinesin proteins in humans Alarge number of these proteins or their orthologues have been shown to possess essential function(s) in both the mitotic and themeiotic cell cycle Kinesins also can be classified into three groups based on the position of their motor domains N-terminalC-terminal and internal kinesins Conventional kinesin operates as a dimer walking in a co-ordinated hand-over-hand fashionalong a microtubule protofilament
Kinesins have important roles in chromosome separation microtubule dynamics spindle formation cytokinesis and cell cycleprogression Roles of kinesins in diseases typically involve defective transport of cell components transport of pathogens or celldivision
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Kinesin Inhibitors
(R)-Filanesib ((R)-ARRY-520) Cat No HY-15187A
(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof Filanesib (HY-15187) Filanesib is a synthetic
inhibitor with ankinesin spindle protein (KSP)IC of 6 nM50
Purity 9886Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ARQ 621Cat No HY-16062
ARQ 621 is an allosteric potent and selectiveinhibitor of a microtubule-based ATPaseEg5motor protein involved in cell divisionAnti-tumor activity ARQ 621 is a kinesininhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
AZ82Cat No HY-12241
AZ82 is a selective kinesin-like protein KIFC1 inhibitor with a of 43 nM and an(HSETKIFC1) Ki
of 300 nM for KIFC1IC50
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
CW-069Cat No HY-15857
CW-069 is an allosteric inhibitor of with an ofmicrotubule motor protein HSET IC50
75 μM
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
DimethylenastronCat No HY-19944
Dimethylenastron is a potent kinesin Eg5inhibitor with an of 200 nMIC50
Purity 9824Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Eg5 Inhibitor V trans-24Cat No HY-112915
Eg5 Inhibitor V trans-24 is a potent and specific inhibitor with an of 065 μM andkinesin Eg5 IC50
can be used in the research of cancer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
EMD534085Cat No HY-15000
EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nMkinesin-5 IC50
Purity 9903Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Filanesib (ARRY-520) Cat No HY-15187
Filanesib (ARRY-520) is a selective andnoncompetitive kinesin spindle protein ( )KSPinhibitor with an of 6 nM for human KSPIC50
Filanesib induces cell death by in vitroapoptosisFilanesib has potent anti-proliferative activity
Purity 9973Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GSK-923295Cat No HY-10299
GSK-923295 is a special allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity with of 32plusmn02Ki
nM and 16plusmn 01 nM for human and caninerespectively
Purity 9956Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
GW406108X (GW108X) Cat No HY-115570
GW406108X is a specific inhibitorKif15 (Kinesin-12)with an of 082 uM in ATPase assaysIC50
GW406108X a potent inhibitor showsautophagyATP competitive inhibition against with aULK1
of 637 (427 nM)pIC50
Purity 9602Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
wwwMedChemExpresscom 21
Ispinesib (SB-715992) Cat No HY-50759
Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app
Purity 9983Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
K858 (Racemic)Cat No HY-19966
K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50
Purity 9993Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Kif15-IN-1Cat No HY-15948
Kif15-IN-1 is an inhibitor of the mitotic Kinesin and is used for thefamily member 15 (Kif15)
research of cellular proliferative diseases
Purity 9953Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Kif15-IN-2Cat No HY-15949
Kif15-IN-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15
proliferative diseases
Purity 9864Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib (LY2523355) Cat No HY-14846
Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity
Purity 9959Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A
Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg
Monastrol ((plusmn)-Monastrol) Cat No HY-101071A
Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50
14 μM
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
PaprotrainCat No HY-101298
Paprotrain is a cell-permeable inhibitor of the inhibits the ATPase activity ofkinesin MKLP-2
MKLP-2 with an of 135 μM and a of 336 μMIC50 Ki
and shows a moderate inhibition activity on with an of 55 μMDYRK1A IC50
Purity 9954Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
PF-2771Cat No HY-19530
PF-2771 is a potent and selective centromere inhibitor inhibiting CENP-Eprotein E (CENP-E)
motor activity with an of 161 nM PF-2771 isIC50
used as an anticancer agent
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-743921Cat No HY-12069
SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki
Purity 9811Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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MicrotubuleTubulin
Microtubules are a component of the cytoskeleton found throughout the cytoplasm These tubular polymers of tubulin can growas long as 50 micrometres with an average length of 25 microm and are highly dynamic The outer diameter of a microtubule is about24 nm while the inner diameter is about 12 nm Microtubules are found in eukaryotic cells and are formed by the polymerization ofa dimer of two globular proteins alpha and beta tubulin Tubulin is one of several members of a small family of globular proteinsThe tubulin superfamily includes five distinct families the alpha- beta- gamma- delta- and epsilon-tubulins and a sixth familywhich is present only in kinetoplastid protozoa The most common members of the tubulin family are α-tubulin and β-tubulin theproteins that make up microtubules Microtubules are very important in a number of cellular processes They are involved inmaintaining the structure of the cell
wwwMedChemExpresscom 23
MicrotubuleTubulin Inhibitors amp Modulators
10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol
10-Deacetylpaclitaxel 7-Xyloside hellip) Cat No HY-20584
10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent enhances tubulinpolymerization) derivative with improvedpharmacological features
Purity gt98Clinical Data No Development ReportedSize 10 mg 50 mg
10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat No HY-N1391
10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus
Zuccwallichiana
Purity ge950Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
10-Oxo Docetaxel (Docetaxel Impurity 1) Cat No HY-16674
10-Oxo Docetaxel (Docetaxel Impurity 1) is a noveltaxoid having remarkable anti-tumor properties anda Docetaxel intermediate
Purity 9804Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
2-Methoxyestradiol (2-ME2 NSC-659853) Cat No HY-12033
2-Methoxyestradiol (2-ME2) an orally activeendogenous metabolite of 17β-estradiol (E2) is an
inducer and an inhibitor withapoptosis angiogenesispotent antineoplastic activity 2-Methoxyestradiolalso destablize microtubules
Purity 9982Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
4-Demethylepipodophyllotoxin (4-O-demethylepipodophyllotoxin 4-DMEP) Cat No HY-17435
4-Demethylepipodophyllotoxin(4-DMEP) is a keyintermediate compound for the preparation ofpodophyllotoxin-type anti-cancer drugs a potentinhibitor of microtubule assembly
Purity 9920Clinical Data No Development ReportedSize 10 mM times 1 mL 50 mg 100 mg
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) Cat No HY-16675
7-Epi-10-oxo-docetaxel (Docetaxel Impurity 2) is aimpurity of docetaxel detected by high performanceliquid chromatography (HPLC)
Purity 9809Clinical Data No Development ReportedSize 1 mg 5 mg
7-Epi-docetaxel (4-epi-Docetaxel 7-Epidocetaxel 7-Epitaxotere) Cat No HY-16676
7-Epi-10-oxo-docetaxel (Docetaxel Impurity C7-Epitaxotere) is a impurity of docetaxel
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 10 mg
7-epi-Taxol (7-epi-Paclitaxel) Cat No HY-N0227
7-epi-Taxol is an active metabolite of taxol withactivity comparable to that of taxol against cellreplication promoting bundlemicrotubuleformation and against microtubuledepolymerization
Purity 9985Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
7-xylosyltaxol (7-Xylosylpaclitaxel Taxol-7-xyloside) Cat No HY-77574
7-xylosyltaxol(Taxol-7-xyloside) is a taxol(Paclitaxel) derivative Paclitaxel binds totubulin and inhibits the disassembly ofmicrotubules
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ABT-751 (E7010) Cat No HY-13270
ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 10 mg 50 mg 100 mg
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AmPEG6C2-Aur0131Cat No HY-111555
AmPEG6C2-Aur0131 is a drug-linker conjugate for (anti-CXCR4 ADC) with potent antitumorADC
activity by using Aur0131 (an auristatinmicrotubule inhibitor) linked via thenon-cleavable linker AmPEG6C2
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Amphethinile (Amphetinile CRC 82-07) Cat No HY-100190
Amphethinile is an agent The affinityanti-tubulinconstant for the association ( ) ofKa
Amphethinile with tubulin is 13 μM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Ansamitocin P 3 (Antibiotic C 15003P3 Maytansinol butyrate) Cat No HY-19839
Ansamitocin P 3 exhibits antitumour activity isan antibody drug conjugate cytotoxin The moreinformation please refer to Ansamitocin P-3(HY-15739 a tubulin inhibitor)
Purity gt98Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Ansamitocin P-3 (Antibiotic C 15003P3 Maytansinol isobutyrate) Cat No HY-15739
Ansamitocin P-3 (Antibiotic C 15003P3) is a inhibitor Ansamitocin P-3 is amicrotubule
macrocyclic antitumor antibiotic
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Auristatin ECat No HY-15582
Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity MMAEanalog and cytotoxin in Antibody-drug conjugatesAuristatin E inhibits cell division by blockingthe polymerisation of tubulin
Purity 9936Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Auristatin FCat No HY-15583
Auristatin F is a potent Auristatin F acytotoxinpotent inhibitor and vascularmicrotubuledamaging agent (VDA) can be used in antibody-drugconjugates (ADC)
Purity 9979Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Batabulin (T138067) Cat No HY-13563
Batabulin (T138067) is an antitumor agent whichbinds covalently and selectively to a subset ofthe thereby disruptingβ-tubulin isotypes
polymerization Batabulin affectsmicrotubulecell morphology and leads to cell-cycle arrestultimately induces cell deathapoptotic
Purity 9991Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Batabulin sodium (T138067 sodium) Cat No HY-13563A
Batabulin sodium (T138067 sodium) is an antitumoragent which binds covalently and selectively to asubset of the thereby disruptingβ-tubulin isotypes
polymerization Batabulin sodiummicrotubuleaffects cell morphology and leads to cell-cyclearrest ultimately induces cell deathapoptotic
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Bis-ANS dipotassiumCat No HY-129811
Bis-ANS dipotassium is a fluorescent probe ofhydrophobic protein Bis-ANS binds to withtubulina of 2 μM Bis-ANS dipotassium is a potentKd
biphasic modulator of protein liquid-liquid phaseseparation ( )LLPS
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
BNC105Cat No HY-16114
BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg
wwwMedChemExpresscom 25
BTB-1Cat No HY-101770
BTB-1 is a potent selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50
of 169 μM
Purity 9969Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cabazitaxel (XRP6258 RPR-116258A taxoid XRP6258) Cat No HY-15459
Cabazitaxel is a semi-synthetic derivative of thenatural taxoid 10-deacetylbaccatin III withpotential antineoplastic activity
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 500 mg
CCB02Cat No HY-114302
CCB02 is a selective CPAP-tubulin interactioninhibitor binding to tubulin and competing forthe CPAP binding site of β-tubulin with an IC50
of 689 nM and shows potent anti-tumor activity
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CephalomannineCat No HY-77554
Cephalomannine is a Paclitaxel (HY-B0015)alkaloidal analog and isolated from most
species Cephalomannine is an orallyCephalotaxusactive and can be used as aanti-tumor agentchemotherapy agent for cancer research
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Ceratamine ACat No HY-N6997
Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge
acts as aPseudoceratina spmicrotubule-stabilizing agent Ceratamine Aexhibits cytotoxicity against human cancer celllines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cevipabulin (TTI-237) Cat No HY-14949
Cevipabulin (TTI-237) is an oralmicrotubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin with3
an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9903Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Cevipabulin fumarate (TTI-237 fumarate) Cat No HY-14949C
Cevipabulin fumarate (TTI-237 fumarate) is anoral microtubule-active antitumor compound andinhibits the binding of [ H]NSC 49842 to tubulin3
with an of 18-40 nM for cytotoxicity in humanIC50
tumor cell line
Purity 9908Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ColchicineCat No HY-16569
Colchicine is a inhibitor and atubulin disrupting agent Colchicinemicrotubule
inhibits microtubule polymerization with an IC50
of 3 nM
Purity 9998Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Combretastatin A4 (CRC 87-09) Cat No HY-N2146
Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 04 μMβ-tubulin Kd
Purity 9943Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 25 mg
Crolibulin (EPC2407) Cat No HY-13603
Crolibulin (EPC2407) is a polymerizationtubulininhibitor with potent induction and cellapoptosisgrowth inhibition Crolibulin has anti-tumoractivity Crolibulin also has cardiovasculartoxicity and neurotoxicity
Purity 9804Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
26 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Cryptophycin 1 (Cryptophycin A) Cat No HY-136294
Cryptophycin 1 is a potent cytotoxicantimicrotubule agent which is isolated from Nostocsp Cryptophycin 1 can induce cells apoptosis andexhibits antitumor activity and exceptionalantiproliferative potency
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CurvulinCat No HY-119692
Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit
assembly and has also been shown tomicrotubuleinhibit iNOS expression
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Cys-mcMMADCat No HY-15750
Cys-mcMMAD is a drug-linker conjugate for ADCMMAD is a potent tubulin inhibitor
Purity gt98Clinical Data No Development ReportedSize 1 mg
D-64131Cat No HY-15482
D-64131 is an orally active inhibitor withtubulinan of 053 μM for tubulin polymerizationIC50
D-64131 has antimitotic activity D-64131 can beused for cancer research
Purity 9917Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
D8-MMAD (Demethyldolastatin 10 D8 Monomethylauristatin D D8
Monomethyl Dolastatin 10 D8) Cat No HY-15581S
D8-MMAD is a deuterated form of MMAD which is a disrupting agentmicrotubule
Purity 9912Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAE (D8-Monomethyl auristatin E) Cat No HY-15162A
D8-MMAE (D8-Monomethyl auristatin E) is adeuterated labeled MMAE a potent mitoticinhibitor and a tubulin inhibitor
Purity 9929Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
D8-MMAF (Monomethylauristatin F D8) Cat No HY-15579S
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride MMAF Hydrochloride a potenttubulin polymerization inhibitor is used as aantitumor agent and a cytotoxic component ofantibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
D8-MMAF hydrochlorideCat No HY-15579AS
D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride which is a microtubuledisrupting agent
Purity 9897Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
DeoxypodophyllotoxinCat No HY-N2500
Deoxypodophyllotoxin (DPT) a derivative ofpodophyllotoxin is a lignan with potentantimitotic anti-inflammatory and antiviralproperties isolated from rhizomes of
(Berberidaceae)Sinopodophullumhexandrum
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg
DM3 (Maytansinoid DM3) Cat No HY-130080
DM3 (Maytansinoid DM3) is a maytansine analogbearing disulfide or thiol groups and a tubulininhibitor and is a cytotoxic moiety of
antibody-drug conjugates (ADCs)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
wwwMedChemExpresscom 27
DM3-SMeCat No HY-130081
DM3-SMe is a maytansine derivative and a tubulininhibitor and is a cytotoxic moiety of
which can beantibody-drug conjugates (ADCs)linked to antibody through disulfide bond orstable thioether bond
Purity gt98Clinical Data No Development ReportedSize 100 mg
DM4Cat No HY-12454
DM4 is is an agent that inhibit cellantitubulindivision DM4 can be used in the preparation ofantibody drug conjugate
Purity 9880Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
DM4-SMeCat No HY-130082
DM4-SMe is a metabolite of antibody-maytansin and a inhibitor andconjugates (AMCs) tubulin
also a cytotoxic moiety of antibody-drug conjugates which can be linked to antibody through(ADCs)
disulfide bond or stable thioether bond DM4-SMeinhibits KB cells with an of 0026 nMIC50
Purity ge980Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg
DM4-SPDPCat No HY-126493
DM4-SPDP is a drug-linker conjugate composed of apotent antitubulin agent DM4 and a linker SMCC tomake antibody drug conjugate
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Docetaxel (RP-56976) Cat No HY-B0011
Docetaxel (RP-56976) is a inhibitormicrotubule depolymerization
with an of 02 μM Docetaxel attenuates theIC50
effects of and gene expressionbcl-2 bcl-xLDocetaxel arrests the cell cycle at G2M and leadsto cell apoptosis
Purity 9996Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg
Docetaxel Trihydrate (RP-56976 Trihydrate) Cat No HY-B0011A
Docetaxel Trihydrate (RP-56976 Trihydrate) is anantineoplastic agent and inhibits
with an microtubule depolymerization IC50
value of 02 μM Docetaxel Trihydrate is asemisynthetic analog of taxol and attenuates the
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg
Dolastatin 10 (DLS 10 NSC 376128) Cat No HY-15580
Dolastatin 10 (DLS 10) is a potent antimitoticpeptide isolated from the marine mollusk Dolabela
that inhibits polymerizationauricularia tubulin
Purity 9852Clinical Data Phase 2Size 1 mg 5 mg
Dolastatin 15 (DLS 15) Cat No HY-P1126
Dolastatin 15 (DLS 15) a depsipeptide derivedfrom is a potentDolabella auricularia
agent structurally related to theantimitoticantitubulin agent Dolastatin 10 Dolastatin 15induces cell cycle arrest and apoptosis inmultiple myeloma cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ELR510444Cat No HY-16191
ELR510444 is a novel microtubule disruptorinhibits MDA-MB-231 cell proliferation with IC50of 309 nM not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines
Purity 9555Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ENMD-1198 (IRC-110160) Cat No HY-16196
ENMD-1198 (IRC-110160) an orally active agent is amicrotubule destabilizing
2-methoxyestradiol analogue with antiproliferativeand antiangiogenic activity
Purity 9887Clinical Data No Development ReportedSize 1 mg
28 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
EntasobulinCat No HY-16777
Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity
Purity 9804Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Epothilone A (Epo A) Cat No HY-13503
Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers3 tubulinwith a of 06-14 μMKi
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg
Epothilone B (EPO 906 Patupilone) Cat No HY-17029
Epothilone B is a stabilizer with amicrotubule of 071μM It acts by binding to the αβ-tubulinKi
heterodimer subunit which causes decreasing ofαβ-tubulin dissociation
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Epothilone D (KOS 862) Cat No HY-15278
Epothilone D (KOS 862) is a potent microtubulestabilizer
Purity 9993Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Eribulin (B1939 E7389 ER-086526) Cat No HY-13442
Eribulin (E7389) is a targetingmicrotubuleagent that is used for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Eribulin mesylate (B1939 mesylate E7389 mesylate ER-086526 mesylate) Cat No HY-13442A
Eribulin mesylate (E7389 mesylate) is a targeting agent that is used formicrotubule
the research of metastatic breast cancer Eribulinmesylate inhibits the proliferation of cancercells by binding microtubule proteins andmicrotubules
Purity 9952Clinical Data LaunchedSize 500 μg 1 mg
Estramustine phosphate sodiumCat No HY-13627
Estramustine phosphate sodium an estradiolanalog is an orally active antimicrotubulechemotherapy agent Estramustine phosphate sodiumdepolymerises by binding tomicrotubulesmicrotubule associated proteins (MAPs) andor totubulin
Purity 9984Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
FlubendazoleCat No HY-B0294
Flubendazole is a safe and efficaciousanthelmintic drug which is widely used foranthelmintic to human rodents and ruminantsFlubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction
Purity 9979Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Flutax-2Cat No HY-131010
FLUTAX-2 is an active fluorescent derivative ofTaxol FLUTAX-2 binds to polymerized αβ-tubulindimers FLUTAX-2 is able to stabilize microtubulesof intact and trophozoitesT gallinae T foetus lt
supgt
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fosbretabulin disodium (CA 4DP CA 4P Combretastatin A4 disodium phosphate) Cat No HY-17449
Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent
Purity 9947Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
wwwMedChemExpresscom 29
Indibulin (ZIO 301 D 24851) Cat No HY-13649
Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity
Purity 9933Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Ixabepilone (BMS-247550 Aza-epothilone B) Cat No HY-10222
Ixabepilone (BMS-247550) is an orallybioavailable inhibitormicrotubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilizationthereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis
Purity 9993Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Lexibulin (CYT-997) Cat No HY-10498
Lexibulin (CYT-997) is a potent and orally active inhibitor with IC50s oftubulin polymerisation
10-100 nM in cancer cell lines with potentcytotoxic and vascular disrupting activity invitro and in vivo
Purity 9808Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
MAP4343Cat No HY-107116
MAP4343 is the 3-methylether derivative ofPregnenolone MAP4343 binds in vitro tomicrotubule-associated protein 2 (MAP2)stimulates the polymerization of tubulin enhancesthe extension of neurites and protects neuronsagainst neurotoxic agents
Purity 9809Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Maytansinol (Ansamitocin P-0) Cat No HY-19474
Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro TargetMicrotubuleTubulin in vitro Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila
Purity 9904Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
MC-Alkyl-Hydrazine Modified MMAFCat No HY-128961
MC-Alkyl-Hydrazine Modified MMAF is a drug-linker with potent antitumor activityconjugate for ADC
by using the Modified MMAF (a tubulin inhibitor)linked via the noncleavable MC-Alkyl-Hydrazine
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MC-betaglucuronide-MMAE-1Cat No HY-136317
MC-betaglucuronide-MMAE-1 is a drug-linker with potent antitumor activityconjugate for ADC
by using MMAE (a tubulin polymerizationinhibitor) linked via the cleavable ADC linkerMC-betaglucuronide
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mc-MMADCat No HY-15740
Mc-MMAD is a protective group(maleimidocaproyl)-conjugated MMAD MMAD is apotent tubulin inhibitor Mc-MMAD is a drug-linkerconjugate for ADC
Purity 9850Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Mc-MMAE (Maleimidocaproyl-monomethylauristatin E) Cat No HY-15741
Mc-MMAE is a protective group(maleimidocaproyl)-conjugated monomethylauristatin E (MMAE) which is a potent tubulininhibitor Mc-MMAE is a drug-linker conjugate forADC
Purity 9647Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
MC-Val-Cit-PAB-MMAFCat No HY-112786
MC-Val-Cit-PAB-MMAF is a drug-linker conjugate for with antitumor activity by using the tubulinADC
inhibitor MMAF linked via cathepsin cleavableMC-Val-Cit-PAB
Purity 9805Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
30 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
McMMAF (Maleimidocaproyl monomethylauristatin F) Cat No HY-15578
McMMAF is a protective group-conjugated MMAF MMAFis a potent tubulin polymerization inhibitor
Purity 9958Clinical Data No Development ReportedSize 1 mg
Mertansine (DM1 Maytansinoid DM1) Cat No HY-19792
Mertansine (DM1) is a inhibitormicrotubulinand is an antibody-conjugatable maytansinoid thatis developed to overcome systemic toxicityassociated with maytansine and to enhancetumor-specific delivery
Purity 9980Clinical Data Phase 2Size 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Microtubule inhibitor 1Cat No HY-114313
Microtubule inhibitor 1 is an antitumor agent with inhibitorymicrotubule polymerization
activity with an value of 9-16 nM in cancerIC50
cells
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mivobulin (NSC 613862 (S)-(-)-NSC 613862) Cat No HY-106423
Mivobulin (NSC 613862) is a inhibitortubulinbinds to tubulin in the region that overlaps thecolchicine site and inhibits tubulinpolymerization Mivobulin (NSC 613862) promotesthe formation of abnormal polymers and a GTPaseactivity in the tubulin dimer
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAD (Demethyldolastatin 10 Monomethylauristatin D
Monomethyl Dolastatin 10) Cat No HY-15581
MMAD is a potent inhibitor is a toxintubulinpayload in antibody drug conjugates ( )ADCs
Purity 9986Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
MMAF (Monomethylauristatin F) Cat No HY-15579
MMAF (Monomethylauristatin F) is a potent tubulin inhibitor and is used as apolymerization
antitumor agent MMAF (Monomethylauristatin F) iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCvorsetuzumab mafodotin and SGN-CD19A
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MMAF hydrochloride (Monomethylauristatin F hydrochloride) Cat No HY-15579A
MMAF (Monomethylauristatin F) hydrochloride is apotent inhibitor and istubulin polymerizationused as a antitumor agent MMAF hydrochloride iswidely used as a cytotoxic component ofantibody-drug conjugates ( s) such asADCVorsetuzumab mafodotin and SGN-CD19A
Purity 9989Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
MMAF sodium (Monomethylauristatin F sodium) Cat No HY-15579B
MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent
Purity gt98Clinical Data No Development ReportedSize 2 mg 5 mg 10 mg
Monomethyl auristatin E (MMAE SGD-1010) Cat No HY-15162
Monomethyl auristatin E (MMAE SGD-1010) is asynthetic derivative of dolastatin 10 andfunctions as a potent inhibitor bymitoticinhibiting polymerizationtubulin
Purity 9992Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg 500 mg 1 g
MPT0B392Cat No HY-101287
MPT0B392 an orally active quinoline derivativeinduces activationc-Jun N-terminal kinase (JNK) leading to apoptosis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 31
MyoseverinCat No HY-W008956
Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments
Purity 990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Nocodazole (Oncodazole R17934) Cat No HY-13520
Nocodazole (Oncodazole) is a rapidly-reversibleinhibitor of Nocodazole binds tomicrotubuleβ-tubulin and disrupts microtubuleassemblydisassembly dynamics which preventsmitosis and induces apoptosis in tumor cells
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
Ombrabulin (AVE8062 AC7700) Cat No HY-14797
Ombrabulin (AVE8062) is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity gt98Clinical Data Phase 3Size 1 mg 5 mg
Ombrabulin hydrochloride (AVE8062 hydrochloride AC7700 hydrochloride) Cat No HY-18256
Ombrabulin hydrochloride is a derivative of CA-4phosphate which is known to exhibit antivasculareffects through selective disruption of the tubulincytoskeleton of endothelial cells
Purity 9984Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
OSIP-486823 (OSIP 486823 OSIP486823 CP248) Cat No HY-U00004
OSIP-486823 is a novel -interferingmicrotubuleagent with distinct biological effects on bothprotein kinase G (PKG) and microtubules
Purity ge980Clinical Data No Development ReportedSize 5 mg
PaclitaxelCat No HY-B0015
Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and
cell death Paclitaxel also inducesapoptoticautophagy
Purity 9997Clinical Data LaunchedSize 10 mM times 1 mL 50 mg 100 mg 500 mg
Parbendazole (SKF 29044) Cat No HY-115364
Parbendazole is a potent inhibitor of assembly destabilizes tubulinmicrotubule
with an of 530nM and exhibits aEC50
broad-spectrum anthelmintic activity
Purity 9901Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
PBOX 6Cat No HY-U00446
PBOX 6 is a pyrrolo-15-benzoxazepine (PBOX)compound acts as a -depolymerizingmicrotubuleagent and an apoptotic agent
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg
PE859Cat No HY-12662
PE859 is a potent inhibitor of both and tau Aβaggregation with values of 066 and 12 μMIC50
respectively
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
PEG4-aminooxy-MMAFCat No HY-128968
PEG4-aminooxy-MMAF is a drug-linker conjugate for with potent antitumor activity by using theADC
potent antitubulin agent MMAF linked via thenoncleavable PEG4
Purity 9720Clinical Data No Development ReportedSize 5 mg 10 mg
32 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
PF-06380101 (Aur0101 Auristatin-0101) Cat No HY-12522
PF-06380101 (Aur0101) an auristatin inhibitor is a cytotoxicmicrotubule
Dolastatin 10 analogue
Purity 9962Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Phomopsin ACat No HY-N6793
Phomopsin A is a cyclic hexapeptide mycotoxinisolated from the fungus Phomopsis
Phomopsin A is aleptostomiformisnoncompetitive inhibitor of the binding ofradiolabeled vincristine to tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PironetinCat No HY-116446
Pironetin is an αβ unsaturated lactone isolatedfrom species Pironetin binds toStreptomyces
and is a potent inhibitor ofα-tubulin polymerization and has cell cyclemicrotubule
arrest and antitumor activity
Purity gt98Clinical Data No Development ReportedSize 1 mg
Plinabulin (NPI-2358) Cat No HY-14444
Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 98 nM against HT-29 cells PlinabulinIC50
binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Podofilox (Podophyllotoxin) Cat No HY-15552
Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II
Purity 9982Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 500 mg
PodophyllotoxoneCat No HY-N2415
Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis
activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S-methyl DM1Cat No HY-100504
S-methyl DM1 is a thiomethyl derivative ofMaytansine S-methyl DM1 binds to with atubulin
of 093 μM and inhibts Kd microtubulepolymerization S-methyl DM1 potently suppresses
dynamic instability and hasmicrotubuleanticancer effects
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
S516Cat No HY-130233
S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 429 μM S516 has markedIC50
antitumor activity
Purity 9803Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Scoulerine ((-)-Scoulerine Discretamine) Cat No HY-N1255
Scoulerine ((-)-Scoulerine) an isoquinolinealkaloid is a potent compoundantimitoticScoulerine is also an inhibitor of (szlig-siteBACE1amyloid precursor protein cleaving enzyme 1)Scoulerine inhibits proliferation arrests cellcycle and induces apoptosis in cancer cells
Purity gt98Clinical Data No Development ReportedSize 5 mg
Soblidotin (Auristatin PE TZT-1027) Cat No HY-14672
Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization
Purity 9964Clinical Data Phase 2Size 1 mg 5 mg 10 mg 25 mg 50 mg
wwwMedChemExpresscom 33
SS28Cat No HY-100761
SS28 a SRT501 analog with oral bioavailabilityinhibits to cause celltubulin polymerizationcycle arrest at G2M phase SS28 results inapoptosis rather than necrosis tubulin
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SSE15206Cat No HY-111425
SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50
overcomes multidrug resistance Causes aberrantmitosis resulting in G2M arrest due to incompletespindle formation in cancer cells
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
T-peptideCat No HY-P2251
T-peptide is a peptide derived from microtubulebinding repeat of Tau protein T-peptideself-assembles into 30-55 nm paired helicalfilaments (PHFs) even in the absense of inducers
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Taccalonolide ACat No HY-N2416
Taccalonolide A is a microtubule stabilizer whichis a steroid isolated from withTacca chantriericytotoxic and antimalarial activitiesTaccalonolide A causes G -M accumulation Bcl-22
phosphorylation and initiation of apoptosis
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taccalonolide AJCat No HY-N4208
Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activitymicrotubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cellswith an IC of 42 nM for HeLa cells50
Purity 9938Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg
Taccalonolide BCat No HY-N3028
Taccalonolide B is microtubule stabilizer isolatedfrom with antitumor activityTacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7)
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg
Taltobulin (HTI-286 SPA-110) Cat No HY-15584
Taltobulin (HTI-286) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin hydrochloride (HTI-286 hydrochloride SPA-110 hydrochloride) Cat No HY-15584B
Taltobulin hydrochloride (HTI-286 hydrochloride)a synthetic analogue of the tripeptidehemiasterlin is a potent agentantimicrotubulethat circumvents P-glycoprotein-mediatedresistance in vitro and in vivo
Purity 9905Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Taltobulin trifluoroacetate (HTI-286 trifluoroacetate SPA-110 trifluoroacetate) Cat No HY-15584A
Taltobulin trifluoroacetate (HTI-286trifluoroacetate) a synthetic analogue of thetripeptide hemiasterlin is a potent
agent that circumventsantimicrotubuleP-glycoprotein-mediated resistance in vitro and invivo
Purity 9996Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
ThiocolchicineCat No HY-116852
Thiocolchicine a derivative modified in the CRing of Colchicine (HY-16569) with enhancedbiological properties Thiocolchicine is a potentinhibitor of ( =25tubulin polymerization IC50
microM) and competitively binds to tubulin with a Ki
of 07 microM
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
34 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Tirbanibulin (KX2-391 KX-01) Cat No HY-10340
Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Srcwith of 9-60 nM in cancer cell linesGI50
Purity 9933Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin dihydrochloride (KX2-391 dihydrochloride KX-01 dihydrochloride) Cat No HY-10340A
Tirbanibulin (dihydrochloride) (KX2-391(dihydrochloride)) is an inhibitor of thatSrctargets the peptide substrate site of Src with
of 9-60 nM in cancer cell linesGI50
Purity 9624Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tirbanibulin Mesylate (KX2-391 Mesylate KX01 Mesylate) Cat No HY-10340B
Tirbanibulin Mesylate (KX2-391 Mesylate) is aninhibitor of that targets the peptideSrcsubstrate site of Src with of 9-60 nM inGI50
cancer cell lines
Purity 9988Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Triclabendazole (CGA89317) Cat No HY-B0621
Triclabendazole(CGA89317) is a benzimidazole itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis
Purity 9838Clinical Data No Development ReportedSize 10 mM times 1 mL 100 mg 500 mg
Tubulin inhibitor 1Cat No HY-112607
Tubulin inhibitor 1 is a inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Tubulin inhibitor 6Cat No HY-136121
Tubulin inhibitor 6 (Compound 14b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 6 inhibitstubulin polymerization with an of 087 μMIC50
Tubulin inhibitor 6 inhibits K562 cell growth withan IC of 840 nM50
Purity 9951Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Tubulin inhibitor 7Cat No HY-136122
Tubulin inhibitor 7 (Compound 33c) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 7 inhibitstubulin polymerization with an of 052 μMIC50
Tubulin inhibitor 7 inhibits K562 cell growth withan IC of 11 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulin inhibitor 8Cat No HY-136123
Tubulin inhibitor 8 (Compound 33b) is a tubulininhibitor and a potent inhibitor of multiplecancer cell lines Tubulin inhibitor 8 inhibitstubulin polymerization with an of 073 μMIC50
Tubulin inhibitor 8 inhibits K562 cell growth withan IC of 14 nM50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
TubulysinCat No HY-128914
Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria
and Archangium geophyra Angiococcusdisciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin A (TubA) Cat No HY-15995
Tubulysin A(TubA) is a myxobacterial product thatcan function as an antiangiogenic agent in many invitro assays anti-microtubule anti-mitotic anapoptosis inducer anticancer anti-angiogenicand antiproliferative
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
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Tubulysin CCat No HY-N2347
Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin DCat No HY-N2348
Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra
Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin ECat No HY-N2346
Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin FCat No HY-N7049
Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin GCat No HY-N7050
Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin HCat No HY-N7051
Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin ICat No HY-N7052
Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 1 mg 5 mg
Tubulysin IM-2Cat No HY-130959
Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin IM-3Cat No HY-130960
Tubulysin IM-3 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Tubulysin MCat No HY-N7053
Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium
and geophyra Angiococcus disciformis
Purity gt98Clinical DataSize 25 mg 50 mg 100 mg
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Valecobulin (CKD-516) Cat No HY-13598
Valecobulin (CKD516) is a valine prodrug of (S516)and a vascular disrupting agent (VDA) Valecobulinis a potent inhibitorβ-tubulin polymerizationwith marked antitumor activity against murine andhuman solid tumors
Purity 9802Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Valecobulin hydrochloride (CKD-516 hydrochloride) Cat No HY-13598A
Valecobulin hydrochloride (CKD-516 hydrochloride)is a valine prodrug of S516 (HY-130233) and avascular disrupting agent (VDA) Valecobulinhydrochloride is a potent β-tubulin
inhibitor with marked antitumorpolymerizationactivity against murine and human solid tumors
Purity 9890Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vat-Cit-PAB-Monomethyl Dolastatin 10Cat No HY-126492
Vat-Cit-PAB-Monomethyl Dolastatin 10 is a with potentdrug-linker conjugate for ADC
antitumor activity by using Monomethyl Dolastatin10 (a potent tubulin inhibitor) linked via theADC linker Vat-Cit-PAB
Purity gt98Clinical Data No Development ReportedSize 10 mg 25 mg 50 mg
Vc-MMADCat No HY-15742
Vc-MMAD consists the ADCs linker (Val-Cit) andpotent tubulin inhibitor (MMAD) Vc-MMAD is adrug-linker conjugate for ADC
Purity 9882Clinical Data No Development ReportedSize 1 mg
VcMMAE (mc-vc-PAB-MMAE) Cat No HY-15575
VcMMAE (mc-vc-PAB-MMAE) is a drug-linker conjugate with potent antitumor activity by usingfor ADC
the anti-mitotic agent monomethyl auristatin E(MMAE a tubulin inhibitor) linked via thelysosomally cleavable dipeptide valine-citrulline(vc)
Purity 9989Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 50 mg 100 mg
VERU-111 (ABI-231) Cat No HY-120599
VERU-111 (ABI-231) is a potent and orally active inhibitor which displays strongα and β tubulin
antiproliferative activity with an average IC of50
52 nM against panels of melanoma and prostatecancer cell lines
Purity gt98Clinical Data No Development ReportedSize 5 mg 10 mg 25 mg 50 mg 100 mg
Verubulin (MPC 6827) Cat No HY-14907
Verubulin (MPC-6827) is a-disrupting agent with potent andmicrotubule
broad-spectrum in vitro and in vivo cytotoxicactivities and acts as a promising candidate forthe treatment of multiple cancer types
Purity 9934Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg
Verubulin hydrochloride (MPC-6827 hydrochloride) Cat No HY-12098
Verubulin hydrochloride (MPC-6827 hydrochloride)is a blood brain barrier permeable
-disrupting agent with potent andmicrotubulebroad-spectrum in vitro and in vivo cytotoxicactivities
Purity 9827Clinical Data Phase 2Size 10 mM times 1 mL 1 mg 5 mg
Vinblastine sulfate (Vincaleukoblastine sulfate salt) Cat No HY-13780
Vinblastine sulfate is a cytotoxic alkaloid usedagainst various cancer types Vinblastine sulfateinhibits the formation of microtubule andsuppresses nAChR with an of 89 μMIC50
Purity 9985Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Vincristine sulfate (Leurocristine sulfate NSC-67574
sulfate 22-Oxovincaleukoblastine sulfate) Cat No HY-N0488
Vincristine sulfate is an antitumor vinca alkaloidwhich inhibits formation in mitoticmicrotubulespindle resulting in an arrest of dividing cellsat the metaphase stage It binds to microtubulewith a of 85 nMKi
Purity 9966Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg 100 mg 200 mg
wwwMedChemExpresscom 37
VindolineCat No HY-N0687
Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly
Purity 9933Clinical Data No Development ReportedSize 5 mg 10 mg 20 mg
Vinflunine ditartrateCat No HY-B0628B
Vinflunine ditartrate is the first fluorinated inhibitor belonging to the Vincamicrotubule
alkaloids family Vinflunine ditartrate hasanti-angiogenic vascular-disrupting andanti-metastatic activities
Purity ge950Clinical Data LaunchedSize 5 mg
Vinorelbine (KW-2307 base) Cat No HY-12053
Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50
of 125 nM
Purity gt98Clinical Data LaunchedSize 10 mg 50 mg
Vinorelbine ditartrate (KW-2307 Nor-5-anhydrovinblastine ditartrate) Cat No HY-12053A
Vinorelbine (ditartrate) is an anti-mitotic agentwhich inhibits the proliferation of Hela cellswith IC of 125 nM50
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 10 mg 50 mg
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Mps1Monopolar spindle 1
Monopolar spindle 1 (Mps1) also known as TTK is a serine threonine kinase which ensures proper biorientation of sisterchromatids on the mitotic spindle by the activation of the spindle assembly checkpoint (SAC) Mps1 has been shown to function asthe key kinase that activates the spindle assembly checkpoint (SAC) to secure proper distribution of chromosomes to daughtercells
Mps1 is a dual specificity protein kinase that is essential for the bipolar attachment of chromosomes to the mitotic spindle and formaintaining the spindle assembly checkpoint until all chromosomes are properly attached Mps1 is expressed at high levels duringmitosis and is abundantly expressed in cancer cells Disruption of Mps1 function induces aneuploidy and cell death
wwwMedChemExpresscom 39
Mps1 Inhibitors
AZ3146Cat No HY-14710
AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50
Mps1 Cat
Purity 9992Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
BAY1217389Cat No HY-12859
BAY 1217389 is a potent and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nMIC50
Purity 9994Clinical Data Phase 1Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg
BOS-172722Cat No HY-112162
BOS-172722 is an inhibitor of monopolar spindle 1(MPS1) checkpoint with an IC of 11 nM and 63 nM50
for MPS1 (1 mM ATP) and P-MPS1 respectivelyBOS-172722 also has potential for the study ofvarious forms of breast cancer
Purity 9941Clinical Data Phase 1Size 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
CCT251455Cat No HY-12603
CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1
of 3 nMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Empesertib (BAY 1161909) Cat No HY-12858
Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
MPI-0479605Cat No HY-12660
MPI-0479605 is a potent and selectiveATP-competitive inhibitor of with an Mps1 IC50
of 18 nM
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg
Mps1-IN-1Cat No HY-13298
Mps1-IN-1 is a potent selective andATP-competitive kinase inhibitor with anMps1
and a of 367 nM and 27 nMIC50 Kd
Purity 9966Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Mps1-IN-1 dihydrochlorideCat No HY-110347
Mps1-IN-1 dihydrochloride is a potent selectiveand ATP-competitive kinase inhibitor withMps1an and a of 367 nM and 27 nMIC50 Kd
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Mps1-IN-2Cat No HY-13994
Mps1-IN-2 is a potent selective andATP-competitive dual inhibitor withMps1Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd
and a of 61 nM for Plk1Kd
Purity 9815Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mps1-IN-3Cat No HY-12401
Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50
Purity ge980Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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NMS-P715Cat No HY-12382
NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50
Purity ge990Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg 100 mg
TC-Mps1-12Cat No HY-110115
TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50
nM
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
wwwMedChemExpresscom 41
Myosin
Myosins are mechanoenzymes that interact with actin filaments and hydrolyse ATP to generate movement and force This enablesmyosins to propel the sliding of actin filaments to produce tension on actin filaments and to walk along these filaments As aresult myosins can regulate the structure and dynamics of the actin cytoskeleton and affect the localization and transport ofcellular components The different myosins are grouped into classes on the basis of their motor domains There are 35 knownclasses of myosin and humans have 40 myosin genes that fall into 13 classes (I II III V VI VII IX X XV XVI XVIII XIX and XXXV)
Myosins are actin-dependent motors that participate in a diverse range of crucial activities including muscle contractionintracellular trafficking cell division motility actin cytoskeletal organisation and cell signaling Myosin malfunction has beenimplicated in a variety of disorders including deafness hypertrophic cardiomyopathy Usher syndrome Griscelli syndrome andcancer
Myosin light chain kinase (MLCK) is an enzyme that activates the myosin light chain to exert its function related to cytoskeletoncontraction and tight junction regulation In most cells MLCK is a transducer for signalling MLC phosphorylation in response to Ca
binding to MLCK-associated calmodulin MLCK-mediated MLC phosphorylation and actomyosin contractility is important in2+
muscle contraction cell migration and endoexocytic processes and is recognized for its central role in signalling endothelialcell-cell adhesion and barrier function
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Myosin Inhibitors Activators amp Modulators
(+)-BlebbistatinCat No HY-107657
(+)-Blebbistatin is the inactive enantiomer of(ndash)-Blebbistatin (ndash)-Blebbistatin is a selectiveinhibitor of myosin II ATPase
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat No HY-13441
(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II
Purity 9942Clinical Data No Development ReportedSize 5 mg 10 mg 50 mg
ATM-3507Cat No HY-100948
ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50
lines
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ATM-3507 trihydrochlorideCat No HY-100948B
ATM-3507 trihydrochloride is a potent inhibitor with s from 383-684tropomyosin IC50
μM in human melanoma cell lines
Purity 9810Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BlebbistatinCat No HY-13813
Blebbistatin is a selective non-muscle myosin inhibitor promotes directionalII (NMII)
migration of corneal endothelial cells (CECs) andaccelerates wound healing and better preservescell junctional integrity and barrier function
Purity 9964Clinical Data No Development ReportedSize 1 mg
BTS (N-Benzyl-p-toluenesulfonamide N-Tosylbenzylamine) Cat No HY-16690
BTS (N-Benzyl-p-toluenesulfonamide) is a potentand selective inhibitor of skeletal muscle myosin
activity with anII subfragment 1 (S1) ATPases of ~5 microM for actin- and Ca -stimulatedIC50
2+
myosin S1 ATPase BTS specifically inhibits thecontraction of fast skeletal muscle fibers
Purity 9978Clinical Data No Development ReportedSize 10 mM times 1 mL 500 mg
Danicamtiv (MYK-491) Cat No HY-109128
Danicamtiv (MYK-491) an inotropic agent is aselective allosteric activator of cardiac
Danicamtiv increases cardiac systolicmyosinfunction and preserves mechanical efficiency
Purity 9949Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
HA-100Cat No HY-100984
HA-100 is an inhibitor of cGMP-dependent proteinkinase ( ) cAMP-dependent protein kinasePKG( ) protein kinase C ( ) and PKA PKC MLC-kinasewith s of 4 8 12 and 240 μM respectivelyIC50
Purity 9977Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Mavacamten (MYK461 SAR439152) Cat No HY-109037
Mavacamten (MYK461) is an orally active modulatorof with of 490 711 nM forcardiac myosin IC s50
bovine cardiac and human cardiac respectively
Purity 9994Clinical Data Phase 3Size 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg
ML-7 hydrochlorideCat No HY-15417
ML-7 hydrochloride is a naphthalene sulphonamidederivative potently inhibits ( =300MLCK IC50
nM) ML-7 hydrochloride also inhibits YAPTAZ
Purity 9975Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
wwwMedChemExpresscom 43
ML-9Cat No HY-100932
ML-9 is a selective and potent inhibitor of Akt inhibits myosin light-chain kinase (MLCK)kinase
and stromal interaction molecule 1 (STIM1)activity ML-9 inhibits inhibits MLCK PKA and PKCactivity with values of 4 32 and 54 μMKi
respectively
Purity 9931Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg 100 mg 250 mg
ML-9 Free BaseCat No HY-100932A
ML-9 (Free Base) is a selective and potentinhibitor of inhibits myosinAkt kinaselight-chain kinase (MLCK) and stromal interactionmolecule 1 (STIM1) activity
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
MLCK inhibitor peptide 18Cat No HY-P1029
MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nMMLCK IC50
and inhibits only at 4000-foldCaM kinase IIhigher concentrations
Purity 9966Clinical Data No Development ReportedSize 1 mg 5 mg 10 mg 25 mg
MS-444 (BE-34776) Cat No HY-100685
MS-444 inhibits the activity of purified smoothmuscle myosin light chain kinase ( ) with anMLCK
value of 10 μMIC50
Purity 9913Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
Omecamtiv mecarbil (CK-1827452) Cat No HY-14233
Omecamtiv mecarbil is a selective cardiac myosinactivator
Purity 9889Clinical Data Phase 3Size 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
para-NitroblebbistatinCat No HY-120870
para-Nitroblebbistatin is a non-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
W-7 hydrochlorideCat No HY-100912
W-7 hydrochloride is a selective calmodulinantagonist W-7 hydrochloride inhibits the
-dependent andCa -calmodulin2+ phosphodiesterase with values of 28myosin light chain kinase IC50
μM and 51 microM respectively W-7 hydrochlorideinduces and has antitumor activityapoptosis
Purity 9965Clinical Data No Development ReportedSize 10 mM times 1 mL 25 mg 50 mg
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PAKp21 activated kinases
PAKs (p21-activated kinases) are key regulators of actin dynamics cell proliferation and cell survival PAKs are SerThr kinases thatare classified into two groups on the basis of their structural and functional features group I (PAK1ndash3) and group II (PAK4ndash6) GroupI PAKs have an auto-inhibitory domain (also called an inhibitory switch domain) and a kinase domain (catalytic domain CD) and areactivated by the binding of the active (that is GTP-bound) forms of Rho GTPases such as Cdc42 and Rac1 Group II PAKs have noauto-inhibitory domains and are not activated by active Rho GTPases Because the deregulation of PAKs is closely associated withvarious human diseasessmall-molecule inhibitors of these kinases have great potential as therapeutic agents In addition thesecompounds can also be used as powerful tools in studies aimed at understanding the PAK signaling pathway
PAKs are considered prime regulators of the actin cytoskeleton and motility Due to their central role in actin remodelling and theirability to activate Matrix metalloproteinases (MMPs) Rho GTPases play an important role in tumor cell invasion and metastasis Thecurrent evidence suggests the involvement of PAKs in motility cell survival anchorage-independent growth angiogenesis invasionmigration and regulation of cell cycle and mitosis Consequently PAKs have also been implicated in a number of pathologicalconditions including cancer
wwwMedChemExpresscom 45
PAK Inhibitors amp Activators
5-Aminosalicylic Acid (Mesalamine 5-ASA Mesalazine) Cat No HY-15027
5-Aminosalicylic acid (Mesalamine) acts as aspecific agonist and also inhibitsPPARγp21-activated kinase 1 ( ) and PAK1 NF-κB
Purity ge980Clinical Data LaunchedSize 10 mM times 1 mL 500 mg
Fingolimod (FTY720 free base) Cat No HY-11063
Fingolimod (FTY720 free base) is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50
0033 nM in K562 and NK cells Fingolimod also isa activator a immunosuppressantpak1
Purity 9981Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
Fingolimod hydrochloride (FTY720) Cat No HY-12005
Fingolimod hydrochloride (FTY720) an analog ofsphingosine is a potent sphingosine 1-phosphate( ) receptors modulator FingolimodS1Phydrochloride is phosphorylated by sphingosinekinases particularly by SK2 and then bindsS1PR1 3 4 and 5
Purity 9986Clinical Data LaunchedSize 10 mM times 1 mL 100 mg 200 mg 500 mg 1 g 5 g
FRAX1036Cat No HY-19538
FRAX1036 is a inhibitor with s of 233 nMPAK Ki
724 nM and 24 μM for PAK1 PAK2 and PAK4respectively
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 50 mg 100 mg
FRAX486Cat No HY-15542B
FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14 33 and 39 nM for PAK1 PAK2 andIC50
PAK3 respectively
Purity 9809Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
FRAX597Cat No HY-15542A
FRAX597 is a potent group I p21-activated Kinases( s) inhibitor with of 8 13 and 19 nM forPAK IC50
and PAK1 2 3
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
G-5555Cat No HY-19635
G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 37 nM and 11 nM for PAK1Ki
and PAK2 respectively
Purity 9918Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg 25 mg 50 mg 100 mg
G-5555 hydrochlorideCat No HY-19635A
G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki
of 37 nM
Purity 9878Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg
GNE 2861Cat No HY-12632
GNE 2861 is a inhibitor that displays groupPAKII selectivity GNE 2861 inhibits PAK4 PAK5 andPAK6 with s of 75 36 126 nM respectivelyIC50
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
IPA-3Cat No HY-15663
IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 25 μM and shows noIC50
inhibition to group II PAKs (PAKs 4-6)
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
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LCH-7749944 (GNF-PF-2356) Cat No HY-125035
LCH-7749944 (GNF-PF-2356) is a potent PAK4inhibitor with an of 1493 μM LCH-7749944IC50
effectively suppresses the proliferation of humangastric cancer cells through downregulation ofPAK4c-SrcEGFRcyclin D1 pathway and induces
apoptosis
Purity 9943Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Mesalamine impurity PCat No HY-131265
Mesalamine impurity P is an impurity of Mesalamine(HY-15027) 5-Aminosalicylic acid (Mesalamine)acts as a specific agonist and alsoPPARγinhibits p21-activated kinase 1 ( )PAK1and NF-κB
Purity gt98Clinical Data No Development ReportedSize 1 mg
NVS-PAK1-1Cat No HY-100519
NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
NVS-PAK1-CCat No HY-131043
NVS-PAK1-C is a potent ATP-competitive andspecific allosteric inhibitor probe withPAK1
values of 5 nM and 6 nM for dephosphorylatedIC50
PAK1 and phosphorylated PAK1 respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
PF-3758309Cat No HY-13007
PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki
Purity 9995Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
PF-3758309 hydrochlorideCat No HY-13007A
PF-3758309 hydrochloride is a potent orallyavailable and reversible ATP-competitiveinhibitor of ( = 27 nM =187 nM)PAK4 Kd Ki
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
wwwMedChemExpresscom 47
ROCKRho-associated protein kinase Rho-associated kinase Rho-kinase ROK
ROCK (Rho-associated protein kinase) is a kinase belonging to the AGC (PKA PKGPKC) family of serine-threonine kinases ROCKs(ROCK1 and ROCK2) occur in mammals zebrafish Xenopus invertebrates and chicken Human ROCK1 has a molecular mass of 158kDa and is a major downstream effector of the small GTPase RhoA Mammalian ROCK consists of a kinase domain acoiled-coilregion and a Pleckstrin homology (PH) domain which reduces the kinase activity of ROCKs by an autoinhibitory intramolecular foldif RhoA-GTP is not present ROCK plays a role in a wide range of different cellular phenomena as ROCK is a downstream effectorprotein of the small GTPase Rho which is one of the major regulators of the cytoskeleton
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ROCK Inhibitors amp Activators
Afuresertib (GSK2110183) Cat No HY-15727
Afuresertib (GSK2110183) is an orallybioavailable selective ATP-competitive andpotent pan-Akt kinase inhibitor with s ofKi
008226 nM for Akt1Akt2Akt3 respectively
Purity 9986Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Afuresertib hydrochloride (GSK2110183 hydrochloride) Cat No HY-15727A
Afuresertib hydrochloride (GSK 2110183hydrochloride) is an orally bioavailableselective ATP-competitive and potent pan-Aktkinase inhibitor with s of 008226 nM forKi
Akt1Akt2Akt3 respectively
Purity 9802Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
AT13148Cat No HY-16071
AT13148 is an orally active and ATP-competitivemulti- inhibitor with s of 38AGC kinase IC50
nM402 nM50 nM 8 nM 3 nM and 6 nM4 nM forAkt123 p70S6K PKA and ROCKIII respectively
Purity 9954Clinical Data Phase 1Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
BDP5290Cat No HY-12437
BDP5290 is a potent inhibitor of both andROCK with s of 5 nM 50 nM 10 nM and 100MRCK IC50
nM for and ROCK1 ROCK2 MRCKα MRCKβrespectively
Purity 9879Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
Belumosudil (KD025 SLx-2119) Cat No HY-15307
Belumosudil (KD025) is a selective inhibitor of with s of 105 nM and 24 microM for ROCK2ROCK2 IC50
and ROCK1 respectively Anti-fibrotic properties
Purity 9977Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
CCG-222740Cat No HY-121750
CCG-222740 is an orally active and selectiveRhomyocardin-related transcription factor
pathway inhibitor CCG-222740 is also a(MRTF)potent inhibitor of alpha-smooth muscle actinprotein expression CCG-222740 effectively reducesfibrosis in skin and blocks melanoma metastasis
Purity 9956Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Chroman 1Cat No HY-15392
Chroman 1 is a highly potent and selective ROCKinhibitor Chroman 1 is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
also has inhibitory activity against withMRCKan of 150 nMIC50
Purity 9990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
Chroman 1 dihydrochlorideCat No HY-15392A
Chroman 1 dihydrochloride is a highly potent andselective inhibitor Chroman 1ROCKdihydrochloride is more potent against ROCK2( =1 pM) than ROCK1 ( =52 pM) Chroman 1IC50 IC50
dihydrochloride also has inhibitory activityagainst with an of 150 nMMRCK IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
CMPD101Cat No HY-103045
CMPD101 is a potent highly selective andmembrane-permeable small-molecule inhibitor of
with of 18 nM and 54 nMGRK23 IC50
respectively
Purity 9868Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg
CRT0066854Cat No HY-18713
CRT0066854 is a potent and selective atypical PKC inhibitor CRT0066854 is againstisoenzymes
full-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity ge990Clinical Data No Development ReportedSize 1 mg
wwwMedChemExpresscom 49
CRT0066854 hydrochlorideCat No HY-18713A
CRT0066854 hydrochloride is a potent and selectiveatypical s inhibitor CRT0066854 is againstPKCfull-length (FL) and kinasesPKCι PKCζ ROCK-IIwith values of 132 nM 639 nM and 620 nMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Fasudil (HA-1077 AT877) Cat No HY-10341A
Fasudil (HA-1077 AT877) is a nonspecific inhibitor and also has inhibitoryRhoAROCK
effect on protein kinases with an of 033 μMKi
for ROCK1 s of 0158 μM and 458 μM 1230IC50
μM 1650 μM for ROCK2 and PKA PKC PKGrespectively
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
Fasudil Hydrochloride (HA-1077 Hydrochloride AT-877 Hydrochloride) Cat No HY-10341
Fasudil Hydrochloride (HA-1077 HydrochlorideAT877 Hydrochloride) is a nonspecific RhoAROCKinhibitor and also has inhibitory effect onprotein kinases with an of 033 μM for ROCK1Ki
s of 0158 μM and 458 μM 1230 μM 1650 μMIC50
for ROCK2 and PKA PKC PKG respectively
Purity 9991Clinical Data LaunchedSize 10 mM times 1 mL 200 mg 500 mg
Glycyl H-1152 hydrochlorideCat No HY-15720B
Glycyl H-1152 hydrochloride (compound 18) is aglycyl derivative of Rho-kinase inhibitors H-1152dihydrochloride Glycyl H-1152 hydrochlorideinhibits and ROCKII Aurora A CAMKII PKGwith s of 00118 235 257 and 326 μMIC50
respectively
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK-25Cat No HY-14362
GSK-25 is a potent selective and orallybioavailable inhibitor ( =7 nM) GSK-25ROCK1 IC50
maintains good selectivity against a panel of 31kinases (gt100 fold) as well as RSK1 and p70S6K(RSK1 IC =398 nM p70S6K IC =1 μM)50 50
Purity 9968Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg
GSK180736ACat No HY-18990
GSK180736A is potent Rho-associated coiled-coil inhibitor with an of 100kinase 1 (ROCK1) IC50
nM GSK180736A is also a selective andATP-competitive G protein-coupled receptor kinase
inhibitor with an of 077 μM2 (GRK2) IC50
Purity 9703Clinical Data No Development ReportedSize 10 mM times 1 mL 2 mg 5 mg 10 mg 50 mg 100 mg
GSK269962A (GSK 269962) Cat No HY-15556
GSK269962A (GSK 269962) is a potent ROCKinhibitor with s of 16 and 4 nM forIC50
recombinant human and respectivelyROCK1 ROCK2GSK269962A has anti-inflammatory and vasodilatoryactivities
Purity 9987Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
GSK269962A hydrochloride (GSK 269962 hydrochloride) Cat No HY-15556A
GSK269962A hydrochloride (GSK 269962hydrochloride) is a potent inhibitor withROCK
s of 16 and 4 nM for recombinant human IC50 ROCK1and respectively GSK269962A hydrochlorideROCK2has anti-inflammatory and vasodilatory activities
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
GSK429286ACat No HY-11000
GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50
Purity 9875Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
H-1152 dihydrochlorideCat No HY-15720A
H-1152 dihydrochloride is a membrane-permeable andselective inhibitor with a value of 16ROCK Ki
nM and an value of 12 nM for IC50 ROCK2
Purity 9932Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg
50 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
HSD1590Cat No HY-126275
HSD1590 is potent inhibitor with s ofROCK IC50
122 and 051 nM for ROCK1 and ROCK2respectively HSD1590 exhibits single digitnanomolar binding to ROCK (K slt2 nM) HSD1590d
displays low cytotoxicity
Purity 9933Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Hydroxyfasudil (HA-1100) Cat No HY-13911
Hydroxyfasudil is a inhibitor with s ofROCK IC50
073 and 072 μM for and ROCK1 ROCK2respectively
Purity 9811Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg
Hydroxyfasudil hydrochloride (HA-1100 hydrochloride HA 1100
hydrochloride HA1100 hydrochloride) Cat No HY-13911A
Hydroxyfasudil hydrochloride is a inhibitorROCKwith s of 073 and 072 μM for andIC50 ROCK1
respectivelyROCK2
Purity 9940Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
LX7101Cat No HY-12659
LX7101 is a potent inhibitor of and LIMK ROCK2with values of 24 16 and 10 nM for LIMK1IC50
LIMK2 and ROCK2 respectively also inhibits PKAwith an less than 1 nMIC50
Purity 9957Clinical Data Phase 2Size 10 mM times 1 mL 2 mg 5 mg 10 mg 25 mg 50 mg 100 mg
Narciclasine (Lycoricidinol) Cat No HY-16563
Narciclasine is a plant growth modulatorNarciclasine modulates the RhoRho kinaseLIMkinasecofilin signaling pathway greatlyincreasing GTPase RhoA activity as well asinducing actin stress fiber formation in aRhoA-dependent manner
Purity 9974Clinical Data No Development ReportedSize 10 mM times 1 mL 1 mg 5 mg 10 mg
Rho-Kinase-IN-1Cat No HY-100270
Rho-Kinase-IN-1 is a inhibitorRho kinase (ROCK)( values of 305 and 39 nM for ROCK1 and ROCK2Ki
respectively) extracted from US20090325960A1compound 1008
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil (K-115) Cat No HY-15685
Ripasudil (K-115) is a specific inhibitor of with s of 19 and 51 nM for andROCK IC50 ROCK2
respectivelyROCK1
Purity 9975Clinical Data LaunchedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
Ripasudil free base (K-115 (free base)) Cat No HY-15685A
Ripasudil free base (K-115 free base) is aspecific inhibitor of with s of 19 andROCK IC50
51 nM for and respectivelyROCK2 ROCK1
Purity gt98Clinical Data LaunchedSize 1 mg 5 mg
RKI-1447Cat No HY-15755
RKI-1447 is a potent small molecule inhibitor of and with values of 145 nM andROCK1 ROCK2 IC50
62 nM respectively
Purity 9806Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK inhibitor-2Cat No HY-119937
ROCK inhibitor-2 is a selective dual andROCK1 inhibitor with s of 17 nM and 2 nMROCK2 IC50
respectively
Purity 9959Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 25 mg 50 mg 100 mg
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ROCK-IN-1Cat No HY-U00351
ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
ROCK-IN-2 (Azaindole 1 TC-S 7001) Cat No HY-10319
ROCK-IN-2 (Azaindole 1 TC-S 7001) is an orallyactive and ATP-competitive inhibitor withROCK
s of 06 and 11nM for human andIC50 ROCK-1 respectivelyROCK-2
Purity 9946Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ROCK2-IN-2Cat No HY-103620
ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
SAR407899Cat No HY-15687A
SAR407899 is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity 9997Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SAR407899 hydrochlorideCat No HY-15687
SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50
135 nM for and s of 36 nM and 41 nM forROCK-2 Ki
human and rat respectivelyROCK-2
Purity ge980Clinical Data Phase 2Size 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
SB-772077B dihydrochlorideCat No HY-108518
SB-772077B dihydrochloride is anaminofurazan-based inhibitorRho kinase (ROCK)with s of 56 nM and 6 nM toward ROCK1 andIC50
ROCK2 respevtively
Purity ge990Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg
SR-3677Cat No HY-13300
SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50
Purity 9991Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg 100 mg
ThiazovivinCat No HY-13257
Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation
Purity 9984Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
Verosudil (AR-12286) Cat No HY-16758
Verosudil (AR-12286) is a potent selective inhibitor with s of 2 and 2 nMRho-kinase (ROCK) Ki
for ROCK1 and ROCK2 respectively AR-12286 lowersintraocular pressure (IOP) primarily by increasingaqueous humour outflow through the trabecularmeshwork
Purity gt98Clinical Data No Development ReportedSize 1 mg 5 mg
Y-27632Cat No HY-10071
Y-27632 is an orally active ATP-competitiveinhibitor of and with s of 220 andROCK-I ROCK-II Ki
300 nM respectively Y-27632 induces apoptosis
Purity 9973Clinical Data No Development ReportedSize 5 mg
52 Tel 609-228-6898 Fax 609-228-5909 Email salesMedChemExpresscom
Y-27632 dihydrochlorideCat No HY-10583
Y-27632 dihydrochloride is an orally activeATP-competitive inhibitor of and ROCK-I ROCK-IIwith s of 220 and 300 nM respectively Y-27632Ki
dihydrochloride induces apoptosis
Purity 9983Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg 200 mg
Y-33075 (Y 39983) Cat No HY-10067
Y-33075 is a selective inhibitor derivedROCKfrom Y-27632 and is more potent than Y-27632with an of 36 nMIC50
Purity 9919Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 50 mg
Y-33075 dihydrochlorideCat No HY-10069
Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50
Purity 9734Clinical Data No Development ReportedSize 10 mM times 1 mL 5 mg 10 mg 50 mg 100 mg
ZINC00881524Cat No HY-101244
ZINC00881524 is a inhibitorROCK
Purity 9941Clinical Data No Development ReportedSize 10 mM times 1 mL 10 mg 25 mg 50 mg 100 mg
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