Cytoskeleton - MedchemExpress.com...Inhibitors, Agonists, Screening Libraries Cytoskeleton The...

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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, Paxillin/FAK 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 Jul;78(3):763-81.[2] Forgacs G, et al. J Cell Sci. 2004 Jun 1;117(Pt 13):2769-75.[3] Eira J, et al. . Prog Neurobiol. 2016 Jun;141:61-82.

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• Arp2/3 Complex 3

• Dynamin 5

• Gap Junction Protein 7

• Integrin 10

• Kinesin 17

• Microtubule/Tubulin 20

• Mps1 34

• Myosin 37

• PAK 40

Inhibitors, Agonists, Screening Librarieswww.MedChemExpress.com

Target List in Cytoskeleton

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Arp2/3 ComplexActin-related protein 2/3 complex

The intact ARP2/3 complex is first purified from based on its affinity for the actin-binding protein profilin,Acanthamoeba 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 ARP2/3 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 70° branch angle. This coupling of nucleation and branching by the ARP2/3 complex isreferred to as autocatalytic branching or dendritic nucleation, and is central to its functions in vivo.

Polymerization of actin filaments directed by the Arp2/3 complex supports many types of cellular movements.


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Arp2/3 Complex Inhibitors

CK-636 (CK-0944636) Cat. No.: HY-15892

CK-636 is a cell permeable inhibitor of Arp2/3, that could inhibit actincomplex

polymerization, with values of 4 μM, 24 μMIC50

and 32 μM for human, fission yeast and bovine,respectively.

Purity: 98.10%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

CK-666Cat. No.: HY-16926

CK-666 is a cell-permeable inhibitor ofactin-related protein , andArp2/3 complexbinds to Arp2/3 complex, stabilizes the inactivestate of the complex, blocking movement of theArp2 and Arp3 subunits into the activatedfilament-like (short pitch) conformation.


CK-869Cat. No.: HY-16927

CK-869 is an Actin-Related Protein 2/3 (ARP2/3)complex inhibitor, with an of 7 μM.IC50

Purity: 99.76%Clinical Data: No Development ReportedSize: 10 mM × 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 filaments,actindisrupting the formation of actin polymers, with

value of 1.4-2.2 nM for F-actin.Kd

Purity: >99.0%Clinical Data: No Development ReportedSize: 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-actin–cofilin interaction by binding to G-actin.

Purity: >99.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg

Dihydrocytochalasin BCat. No.: HY-N6701

Dihydrocytochalasin B (H2CB) is a Cytokinesisinhibitor and changes the morphology of the cells,similar to that of cytochalasin B; does notinhibit glucose transport.

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg

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 actin,with s of 0.1, 0.4, 4.7 μM and 0.19 μM forKd

ATP-actin, ADP-Pi-actin, ADP-actin and G-actin,respectively.

Purity: >95.0%Clinical Data: No Development ReportedSize: 100 μg (0.2 mM * 1 mL in Ethanol),


https://www.MedChemExpress.com/Targets/Arp2/3 Complex.html

https://www.MedChemExpress.com/CK-636.html

https://www.MedChemExpress.com/ck-666.html

https://www.MedChemExpress.com/CK-869.html

https://www.MedChemExpress.com/Cytochalasin_B.html

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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),S.cerevisiae 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

DynasoreCat. No.: HY-15304

Dynasore is a cell-permeable inhibitordynaminwith an of 15 μM.IC50

Purity: 99.61%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 10 mg, 50 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/ inhibitor.mitophagy

Purity: 98.75%Clinical Data: No Development ReportedSize: 10 mM × 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: >99.0%Clinical Data: No Development ReportedSize: 10 mM × 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 (e.g. c-AMP,inositol 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 processes.Formation of GJIC is an essential mechanism in coordinating growth and development and tissue compartmentalization duringembryonic development.


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Gap Junction Protein Inhibitors & Modulators

AT-1002Cat. No.: HY-114426

AT-1002, a 6-mer synthetic peptide, is a tight regulator and absorption enhancer.junction


AT-1002 TFACat. No.: HY-114426A

AT-1002 TFA, a 6-mer synthetic peptide, is a tight regulator and absorption enhancer.junction


Danegaptide (GAP-134; ZP 1609) Cat. No.: HY-10913

Danegaptide (GAP-134), a small modified dipeptide,has been identified as a potent and selectivesecond generation gap junction modifier with oralbioavailability.

Purity: >98%Clinical 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 selective modifier of the gap junctionprotein.

Purity: 99.75%Clinical Data: Phase 2Size: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg

Gap 26Cat. No.: HY-P1082

Gap 26 is a connexin mimetic peptide correspondingto the residues 63-75 of connexin 43, which is a

blocker.gap junction

Purity: 99.30%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg

Gap 27Cat. No.: HY-P0139

Gap 27, connexin43 mimetic peptide, is a gap inhibitor.junction

Purity: 98.34%Clinical 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.


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.


Larazotide acetateCat. No.: HY-106268A

Larazotide acetate is a synthetic peptide thatfunctions as a tight junction regulator andreverses leaky junctions to their normally closedstate.

Purity: 99.68%Clinical Data: Phase 2Size: 10 mM × 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).



https://www.MedChemExpress.com/Targets/Gap Junction Protein.html

https://www.MedChemExpress.com/AT-1002.html

https://www.MedChemExpress.com/AT-1002_TFA.html

https://www.MedChemExpress.com/gap-134.html

https://www.MedChemExpress.com/GAP-134-Hydrochloride.html

https://www.MedChemExpress.com/Gap_26.html

https://www.MedChemExpress.com/Gap_27.html

https://www.MedChemExpress.com/gap19.html

https://www.MedChemExpress.com/gap19-tfa.html

https://www.MedChemExpress.com/Larazotide_acetate.html

https://www.MedChemExpress.com/meclofenamate-sodium.html

Meclofenamic acidCat. No.: HY-117275

Meclofenamic acid is a nonsteroidalanti-inflammatory drug (NSAID) approved for use inarthritis (osteo and rheumatoid), analgesia (mildto moderate pain), dysmenorrhea, and heavymenstrual blood loss (menorrhagia).


Tonabersat (SB-220453) Cat. No.: HY-15204

Tonabersat is a modulator.gap-junction



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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 family,including 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 signaling,including the PI3K/Akt- and Ras/MAPK-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 state.Based 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, Antagonists & Modulators

Arg-Gly-Asp-Ser (RGDS peptide; Fibronectin tetrapeptide) Cat. No.: HY-12290

Arg-Gly-Asp-Ser is an integrin binding sequencethat inhibits function,integrin receptordecreases systemic inflammation via inhibition ofcollagen-triggered activation of leukocytes andattenuates expression of inflammatory cytokines,iNOS and MMP-9.


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 function.integrin 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: >98%Clinical Data:Size: 1 mg, 5 mg

ATN-161Cat. No.: HY-13535

ATN-161 is a novel antagonist, whichintegrin α5β1inhibits angiogenesis and growth of livermetastases in a murine model.

Purity: >98%Clinical Data: Phase 2Size: 5 mg, 10 mg, 50 mg, 100 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: >95.0%Clinical 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.


BMS-688521Cat. No.: HY-10596

BMS-688521 is a highly potent, orally activeinhibitor of the interaction, withLFA-1/ICAMan of 2.5 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: >98%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg

c(phg-isoDGR-(NMe)k)Cat. No.: HY-111413

c(phg-isoDGR-(NMe)k) is a selective and potent ligand with an of 2.9 nM.α5β1-integrin IC50

Purity: >98%Clinical 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 2.9 nM.α5β1-integrin IC50

Purity: >98%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 1 mg, 5 mg, 10 mg

CarotegrastCat. No.: HY-14857

Carotegrast is an orally available α4 integrin inhibitor with anti-inflammatoriesreceptor

activities.


Cilengitide (EMD 121974) Cat. No.: HY-16141

Cilengitide is a potent and selective integrininhibitor for α β and α β receptor, withv 3 v 5

s of 4 and 79 nM, respectively.IC50



https://www.MedChemExpress.com/Targets/Integrin.html

https://www.MedChemExpress.com/Arg-Gly-Asp-Ser.html

https://www.MedChemExpress.com/arg-gly-asp-ser-tfa.html

https://www.MedChemExpress.com/atn-161.html

https://www.MedChemExpress.com/ATN-161-trifluoroacetate-salt.html

https://www.MedChemExpress.com/bi-1950.html

https://www.MedChemExpress.com/bms-688521.html

https://www.MedChemExpress.com/c_phg-isoD-G-R-_NMe_k_.html

https://www.MedChemExpress.com/c-phg-isod-g-r-nme-k-tfa.html

https://www.MedChemExpress.com/Carotegrast.html

https://www.MedChemExpress.com/Cilengitide.html

Cucurbitacin BCat. No.: HY-N0416

Cucurbitacin B belongs to a class of highlyoxidized tetracyclic triterpenoids; could represscancer cell progression.


CWHM-12Cat. No.: HY-18644

CWHM-12 is a potent inhibitor of withαV integrinss of 0.2, 0.8, 1.5, and 1.8 nM for ,IC50 αvβ8

, , and .αvβ3 αvβ6 αvβ1


Cyclo(-RGDfK)Cat. No.: HY-P0023

Cyclo(-RGDfK) is a potent and selective inhibitorof the integrin, with an of 0.94 nM.α βv 3 IC50

Purity: >98.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

Cyclo(Arg-Gly-Asp-D-Phe-Val) TFACat. No.: HY-P1613A

Cyclo(Arg-Gly-Asp-D-Phe-Val) (TFA) is an inhibitorof , with antitumor activity.integrin αvβ3

Purity: 99.40%Clinical 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: 98.03%Clinical 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 nM.integrin IC50

Purity: >98%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 25 mg, 50 mg, 100 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.


E7820 (ER68203-00) Cat. No.: HY-14571

E7820 is an angiogenesis inhibitor by suppressing, a cell adhesion molecule expressed onintegrin a2

endothelial cells.


EptifibatideCat. No.: HY-B0686

Eptifibatide is a cyclic heptapeptide, acts as acompetitive antagonist for the activated platelet

, with anti-plateletglycoprotein IIb/IIIa receptoractivity.

Purity: 96.49%Clinical Data: LaunchedSize: 10 mM × 1 mL, 10 mg, 50 mg, 100 mg

Firategrast (SB 683699) Cat. No.: HY-14951

Firategrast is an orally bioavailable /α4β1 α4β7 antagonist.integrin



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https://www.MedChemExpress.com/E7820.html

https://www.MedChemExpress.com/Eptifibatide.html

https://www.MedChemExpress.com/Firategrast.html

Fradafiban (BIBU-52) Cat. No.: HY-101720

Fradafiban is a nonpeptide platelet glycoproteinIIb/IIIa antagonist, which binds to the humanplatelet GP IIb/IIIa complex with a K value ofd

148 nM.


GLPG0187Cat. No.: HY-100506

GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity; inhibitsα β -integrin with an of 1.3 nM.v 1 IC50

Purity: 98.97%Clinical Data: Phase 1Size: 10 mM × 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 glycoprotein,osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrinreceptors αvβ3 and αvβ5 with estimated of 5IC50

and 6.5 μM.

Purity: 98.12%Clinical 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 glycoprotein,osteopontin. Gly-Arg-Gly-Asp-Ser binds to integrin

αvβ3 and αvβ5 with estimated of 5receptors IC50

and 6.5 μM.


GRGDSPCat. No.: HY-P0290

GRGDSP, a synthetic linear RGD peptide, is an inhibitor.integrin


GRGDSP TFACat. No.: HY-P0290A

GRGDSP (TFA) is an inhibitor.integrin


ILK-IN-2 (OSU-T315 analog) Cat. No.: HY-18676B

ILK-IN-2 (OSU-T315 analog) is a ILK inhibitor.


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.


Integrin-IN-2Cat. No.: HY-130119

Integrin-IN-2 (compound 39) is an orallybioavailable pan inhibitor.αv integrinIntegrin-IN-2 can increases the , ,αvβ6 αvβ3

and binding affinities with αvβ5 αvβ8 pIC50

values of 7.8, 8.4, 8.4 and 7.4, respectively.


iRGD peptide (c(CRGDKGPDC)) Cat. No.: HY-P0122

iRGD peptide is a 9-amino acid cyclic peptide,triggers tissue penetration of drugs by firstbinding to , then proteolyticallyav integrinscleaved in the tumor to produce CRGDK/R tointeract with neuropilin-1, and hastumor-targeting and tumor-penetrating properties.



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https://www.MedChemExpress.com/Integrin-Antagonists-27.html

https://www.MedChemExpress.com/integrin-in-2.html

https://www.MedChemExpress.com/iRGD_peptide.html

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.


Lifitegrast (SAR 1118; SHP-606) Cat. No.: HY-19344

Lifitegrast (SAR 1118) is an integrin lymphocytefunction-associated antigen-1 ( ) antagonist;LFA-1inhibits Jurkat T cell attachment to ICAM-1with an of 2.98 nM.IC50

Purity: 99.58%Clinical Data: LaunchedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg, 200 mg

LXW7Cat. No.: HY-P0178

LXW7 is an octamer disulfide cyclic peptide, alsoa ligand, acts as a potent andαvβ3 integrinspecific endothelial progenitor cells (EPCs) andendothelial cells (ECs) targeting ligand. LXW7increases phosphorylation of VEGFR-2 andactivation of ERK1/2.


MK-0429 (L-000845704) Cat. No.: HY-15102

MK-0429 (L-000845704) is an orally active, potent,selective and nonpeptide antagonistαvβ3 integrinwith an of 80 nM.IC50


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 Crohn's disease.


OSU-T315Cat. No.: HY-18676

OSU-T315 (ILK-IN-1) is a small Integrin-linkedkinase inhibitor with an IC of 0.6 μM,(ILK) 50

inhibiting PI3K/AKT signaling by dephosphorylationof AKT-Ser473 and other ILK targets (GSK-3β andmyosin light chain).


RGDCat. No.: HY-P0278

RGD is a tripeptide that effectively triggers celladhesion, addresses certain cell lines and elicitsspecific cell responses; binds to .integrins

Purity: >98%Clinical Data: Phase 2Size: 5 mg, 10 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, migration,growth, and differentiation.


RGD peptide GRGDNPCat. No.: HY-P1740

RGD peptide (GRGDNP) acts as an inhibitor ofintegrin-ligand interactions and plays animportant role in cell adhesion, migration,growth, and differentiation.


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: >98.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg


https://www.MedChemExpress.com/irigenin.html

https://www.MedChemExpress.com/Lifitegrast.html

https://www.MedChemExpress.com/lxw7.html

https://www.MedChemExpress.com/MK-0429.html

https://www.MedChemExpress.com/natalizumab.html

https://www.MedChemExpress.com/ILK-IN-1.html

https://www.MedChemExpress.com/RGD.html

https://www.MedChemExpress.com/rgd-peptide-grgdnp-tfa.html

https://www.MedChemExpress.com/rgd-peptide.html

https://www.MedChemExpress.com/RGD_Trifluoroacetate.html

RisuteganibCat. No.: HY-P1930

Risuteganib is an anti-integrin that downregulatesoxidative stress and restores homeostasis, andtargets three integrin receptors that areimplicated in dry age-related macular degeneration(AMD) in order to restore homeostasis in theretina .

Purity: >98%Clinical Data: No Development ReportedSize: 100 mg

RWJ 50271Cat. No.: HY-110086

RWJ 50271 is an selective inhibitor oflymphocyte function-associatedantigen-1/intercellular adhesion

interaction with anmolecule-1(LFA-1/ICAM-1) of 5.0 μM (HL60 cells).IC50

Purity: >99.0%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg

SR121566ACat. No.: HY-U00235

SR121566A is a novel non-peptide Glycoprotein ( ) antagonist, which canIIb/IIIa GP IIb-IIIa

inhibit ADP-, arachidonic acid- andcollagen-induced human platelet aggregation with

s of 46±7.5, 56±6 and 42±3 nM, respectively.IC50

Purity: >98%Clinical Data: No Development ReportedSize: 1 mg, 5 mg, 10 mg, 20 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 4.4 nM.CD49d/CD29) IC50

Purity: >99.0%Clinical Data: No Development ReportedSize: 5 mg

Tirofiban (L700462; MK383) Cat. No.: HY-17369B

Tirofiban(L700462;MK383) is a potent non-peptide,glycoprotein IIb/IIIa (integrins alphaIIbbetaIII)antagonist Target: integrin IIb/IIIa Tirofibanhydrochloride monohydrate blocks plateletaggregation and thrombus formation.

Purity: >98%Clinical Data: LaunchedSize: 5 mg, 10 mg

Tirofiban hydrochloride monohydrateCat. No.: HY-17369

Tirofiban hydrochloride monohydrate is a potentnon-peptide, glycoprotein IIb/IIIa (integrinsalphaIIbbetaIII) antagonist IC50 value: Target:integrin IIb/IIIa Tirofiban hydrochloridemonohydrate blocks platelet aggregation andthrombus formation.

Purity: 99.99%Clinical Data: LaunchedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

TR-14035Cat. No.: HY-15770

TR-14035 is a a dual alpha4beta7(IC50=7nM)/alpha4beta1 (IC50=87 nM) integrin antagonist .


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 Crohn's disease.

Purity: 99.64%Clinical Data: LaunchedSize: 1 mg, 5 mg

Zaurategrast (CT7758) Cat. No.: HY-70073

Zaurategrast (CT7758) is a potent andoral-effective inhibitor.α -integrin4


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.



https://www.MedChemExpress.com/risuteganib.html

https://www.MedChemExpress.com/rwj-50271.html

https://www.MedChemExpress.com/SR121566A.html

https://www.MedChemExpress.com/tcs-2314.html

https://www.MedChemExpress.com/tirofiban.html

https://www.MedChemExpress.com/Tirofiban-hydrochloride-monohydrate.html

https://www.MedChemExpress.com/TR-14035.html

https://www.MedChemExpress.com/Vedolizumab.html

https://www.MedChemExpress.com/zaurategrast.html

https://www.MedChemExpress.com/Zaurategrast_ethyl_ester.html

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.


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.


α2β1 Integrin Ligand Peptide (TFA)Cat. 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.


αvβ1 integrin-IN-1Cat. No.: HY-100445

αvβ1 integrin-IN-1 (Compound C8) is a potent andselective inhibitor with an ofαvβ1 integrin IC50

0.63 nM. Antifibrotic effects.



https://www.MedChemExpress.com/Zaurategrast_ethyl_ester_sulfate.html

https://www.MedChemExpress.com/alpha-2-beta-1-integrin-ligand-peptide.html

https://www.MedChemExpress.com/alpha-2-beta-1-integrin-ligand-peptide-tfa.html

https://www.MedChemExpress.com/v1-integrin-in-1.html

Kinesin

Kinesin is a protein belonging to a class of motor proteins found in eukaryotic cells. Kinesins move along microtubule filaments,and are powered by the hydrolysis of ATP (thus kinesins are ATPases). The active movement of kinesins supports several cellularfunctions including mitosis, meiosis and transport of cellular cargo. Most kinesins walk towards the plus end of a microtubule,entails transporting cargo from the centre of the cell towards the periphery. Kinesins were discovered as microtubule (MT)-basedanterograde intracellular transport motors. The founding member of this superfamily, the genomes of mammals encode more than40 kinesin proteins, organized into at least 14 families named kinesin-1 through kinesin-14.


https://www.MedChemExpress.com/Targets/Kinesin.html

Kinesin Inhibitors

(R)-Filanesib ((R)-ARRY-520) Cat. No.: HY-15187A

(R)-Filanesib ((R)-ARRY-520) is the R-enantiomerof ARRY-520. (R)-Filanesib ((R)-ARRY-520) is asynthetic inhibitorkinesin spindle protein (KSP)with of 6 nM.IC50


AZ82Cat. No.: HY-12241

AZ82 is a selective kinesin-like protein KIFC1 inhibitor, with a of 43 nM and an(HSET/KIFC1) Ki

of 300 nM for KIFC1.IC50

Purity: 99.08%Clinical Data: No Development ReportedSize: 10 mM × 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.


DimethylenastronCat. No.: HY-19944

Dimethylenastron is a potent kinesin Eg5inhibitor, with an of 200 nM.IC50


Eg5 Inhibitor V, trans-24Cat. No.: HY-112915

Eg5 Inhibitor V, trans-24 is a potent and specific inhibitor with an of 0.65 μM, andkinesin Eg5 IC50

can be used in the research of cancer.


EMD534085Cat. No.: HY-15000

EMD534085 is a potent and selective inhibitor ofthe mitotic with an of 8 nM.kinesin-5 IC50


Filanesib (ARRY-520) Cat. No.: HY-15187

Filanesib (ARRY-520) is a synthetic kinesin spindle inhibitor with of 6 nM.protein (KSP) IC50


GSK-923295Cat. No.: HY-10299

GSK-923295 is a special, allosteric inhibitor ofcentromere-associated protein-E (CENP-E)kinesin motor ATPase activity, with of 3.2±0.2Ki

nM and 1.6± 0.1 nM for human and canine,respectively.


Ispinesib (SB-715992) Cat. No.: HY-50759

Ispinesib is a specific inhibitor of kinesin, with a of 1.7 nM.spindle protein (KSP) Ki app


K858 (Racemic)Cat. No.: HY-19966

K858 Racemic is an ATP-uncompetitive inhibitor of with an of 1.3 μM.kinesin Eg5 IC50



https://www.MedChemExpress.com/Targets/Kinesin.html

https://www.MedChemExpress.com/arry-520-r-enantiomer.html

https://www.MedChemExpress.com/AZ82.html

https://www.MedChemExpress.com/CW-069.html

https://www.MedChemExpress.com/Dimethylenastron.html

https://www.MedChemExpress.com/Eg5_Inhibitor_V,_trans-24.html

https://www.MedChemExpress.com/EMD534085.html

https://www.MedChemExpress.com/ARRY-520.html

https://www.MedChemExpress.com/GSK-923295.html

https://www.MedChemExpress.com/Ispinesib.html

https://www.MedChemExpress.com/K858.html

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.


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.


Litronesib (LY-2523355; KF-89617) Cat. No.: HY-14846

Litronesib is a selective mitosis-specific kinesin inhibitor, with antitumor activity.Eg5


Litronesib Racemate (LY-2523355 Racemate; KF-89617 Racemate) Cat. No.: HY-14846A

Litronesib (Racemate) is the racemate oflitronesib. Litronesib is a selective, allostericinhibitor of .kinesin Eg5


Monastrol ((±)-Monastrol) Cat. No.: HY-101071A

Monastrol is a potent and cell-permeable inhibitorof the mitotic with an value ofkinesin Eg5 IC50

14 μM.


PaprotrainCat. No.: HY-101298

Paprotrain is a cell-permeable inhibitor of the, inhibits the ATPase activity ofkinesin MKLP-2

MKLP-2 with an of 1.35 μM and a of 3.36 μMIC50 Ki

and shows a moderate inhibition activity on with an of 5.5 μM.DYRK1A IC50


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 16.1 nM; PF-2771 isIC50

used as an anticancer agent.


SB-743921Cat. No.: HY-12069

SB-743921 is a potent inhibitor of the mitotic, with a of 0.1 nM.kinesin KSP (Eg5) Ki



https://www.MedChemExpress.com/kif15-in-1.html

https://www.MedChemExpress.com/kif15-in-2.html

https://www.MedChemExpress.com/Litronesib.html

https://www.MedChemExpress.com/Litronesib-Racemate.html

https://www.MedChemExpress.com/Monastrol.html

https://www.MedChemExpress.com/Paprotrain.html

https://www.MedChemExpress.com/PF-2771.html

https://www.MedChemExpress.com/SB-743921.html

Microtubule/Tubulin

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 µm, 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 proteins.The 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.


https://www.MedChemExpress.com/Targets/Microtubule_Tubulin.html

Microtubule/Tubulin Inhibitors & Modulators

10-Deacetyl-7-xylosyl paclitaxel (10-Deacetyl-7-xylosyltaxol;

10-Deacetylpaclitaxel 7-Xyloside; …) Cat. No.: HY-20584

10-Deacetyl-7-xylosyl paclitaxel is a Paclitaxel(a microtubule stabilizing agent; enhances tubulinpolymerization) derivative with improvedpharmacological features.


10-Deacetyltaxol (10-Deacetylpaclitaxel) Cat. No.: HY-N1391

10-Deacetyltaxol (10-Deacetylpaclitaxel) is ataxane derivative isolated from Taxus

Zucc.wallichiana


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.


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


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.


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: >98.0%Clinical 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 C;7-Epitaxotere) is a impurity of docetaxel.


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.


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.


ABT-751 (E7010) Cat. No.: HY-13270

ABT-751(E 7010) is a novel bioavailabletubulin-binding and antimitotic sulfonamide agentwith IC50 of about 1.5 and 3.4 μM in neuroblastomaand non-neuroblastoma cell lines, respectively.



https://www.MedChemExpress.com/Targets/Microtubule/Tubulin.html

https://www.MedChemExpress.com/10-deacetyl-7-xylosyl-paclitaxel.html

https://www.MedChemExpress.com/10-deacetyltaxol.html

https://www.MedChemExpress.com/10-oxo-docetaxel.html

https://www.MedChemExpress.com/2-Methoxyestradiol.html

https://www.MedChemExpress.com/4_acute_-demethylepipodophyllotoxin.html

https://www.MedChemExpress.com/7-epi-10-oxo-docetaxel.html

https://www.MedChemExpress.com/7-Epi-docetaxel.html

https://www.MedChemExpress.com/7-epi-Taxol.html

https://www.MedChemExpress.com/7-xylosyltaxol.html

https://www.MedChemExpress.com/ABT-751.html

AcLys-PABC-VC-Aur0101Cat. No.: HY-111554

AcLys-PABC-VC-Aur0101 is a drug-linker conjugate (anti-CXCR4 ADC) with potent antitumorfor ADC

activity by using Aur0101 (an auristatinmicrotubule inhibitor), linked via the cleavablelinker AcLys-PABC-VC.


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.


Amphethinile (Amphetinile; CRC 82-07) Cat. No.: HY-100190

Amphethinile is an agent. The affinityanti-tubulinconstant for the association ( ) ofKa

Amphethinile with tubulin is 1.3 μM.


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).


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.


Auristatin ECat. No.: HY-15582

Auristatin E is a cytotoxic tubulin modifier withpotent and selective antitumor activity; MMAEanalog and cytotoxin in Antibody-drug conjugates.Auristatin E inhibits cell division by blockingthe polymerisation of tubulin.


Auristatin FCat. No.: HY-15583

Auristatin F is a cytotoxic tubulin modifier withpotent and selective antitumor activity; MMAFanalog and cytotoxin in Antibody-drug conjugates.Auristatin F inhibits cell division by blockingthe polymerisation of tubulin.


BNC105Cat. No.: HY-16114

BNC105 is a tubulin polymerization inhibitor withpotent antiproliferative and tumor vasculardisrupting properties.


BTB-1Cat. No.: HY-101770

BTB-1 is a potent, selective and reversiblemitotic motor protein inhibitor with an Kif18A IC50

of 1.69 μM.


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.



https://www.MedChemExpress.com/AcLys-PABC-VC-Aur0101.html

https://www.MedChemExpress.com/AmPEG6C2-Aur0131.html

https://www.MedChemExpress.com/Amphethinile.html

https://www.MedChemExpress.com/Ansamitocin-P-3_acute_.html

https://www.MedChemExpress.com/Ansamitocin-P-3.html

https://www.MedChemExpress.com/Auristatin-E.html

https://www.MedChemExpress.com/Auristatin-F.html

https://www.MedChemExpress.com/BNC105.html

https://www.MedChemExpress.com/BTB-1.html

https://www.MedChemExpress.com/Cabazitaxel.html

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.


CephalomannineCat. No.: HY-77554

Cephalomannine is a taxol derivative withantitumor, antiproliferative properties.


Ceratamine ACat. No.: HY-N6997

Ceratamine A is an antimitotic heterocyclicalkaloid isolated from the marine sponge

, acts as aPseudoceratina sp.microtubule-stabilizing agent. Ceratamine Aexhibits cytotoxicity against human cancer celllines.


Cevipabulin (TTI-237) Cat. No.: HY-14949

Cevipabulin (TTI-237) is an oral,microtubule-active antitumor compound and inhibitsthe binding of [ H] vinblastine to tubulin, with3

an of 18-40 nM for cytotoxicity in humanIC50

tumor cell line.


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 tubulin,3

with an of 18-40 nM for cytotoxicity in humanIC50

tumor cell line.


ColchicineCat. No.: HY-16569

Colchicine is a inhibitor and atubulin disrupting agent. Colchicinemicrotubule

inhibits microtubule polymerization with an IC50

of 3 nM.

Purity: 99.98%Clinical Data: LaunchedSize: 10 mM × 1 mL, 200 mg, 500 mg

Combretastatin A4 (CRC 87-09) Cat. No.: HY-N2146

Combretastatin A4 is a -targetingmicrotubuleagent that binds with of 0.4 μM.β-tubulin Kd


Crolibulin (EPC2407) Cat. No.: HY-13603

Crolibulin is a small molecule tubulin inhibitor.polymerization


Cys-mcMMADCat. No.: HY-15750

Cys-mcMMAD is a drug-linker conjugate for ADC.MMAD is a potent tubulin inhibitor.


D-64131Cat. No.: HY-15482

D-64131 is a novel inhibitor of Tubulinpolymerization that competitively binds with[(3)H]colchicine to αβ-Tubulin.



https://www.MedChemExpress.com/CCB02.html

https://www.MedChemExpress.com/cephalomannine.html

https://www.MedChemExpress.com/ceratamine-a.html

https://www.MedChemExpress.com/Cevipabulin.html

https://www.MedChemExpress.com/Cevipabulin_fumarate.html

https://www.MedChemExpress.com/Colchicine.html

https://www.MedChemExpress.com/Combretastatin-A4.html

https://www.MedChemExpress.com/Crolibulin.html

https://www.MedChemExpress.com/cys-mcmmad.html

https://www.MedChemExpress.com/D-64131.html

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 agent.microtubule


D8-MMAE (D8-Monomethyl auristatin E) Cat. No.: HY-15162A

D8-MMAE is a deuterated labeled MMAE, a potent inhibitor and a tubulin inhibitor.mitotic


D8-MMAF (Monomethylauristatin F D8) Cat. No.: HY-15579S

D8-MMAF is a deuterated form of MMAF, which is a disrupting agent.microtubule


D8-MMAF hydrochlorideCat. No.: HY-15579AS

D8-MMAF hydrochloride is a deuterated form of MMAFhydrochloride, which is a microtubuledisrupting agent.


DeoxypodophyllotoxinCat. No.: HY-N2500

Deoxypodophyllotoxin (DPT), a derivative ofpodophyllotoxin, is a lignan with potentantimitotic, anti-inflammatory and antiviralproperties isolated from rhizomes of

(Berberidaceae).Sinopodophullumhexandrum


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)


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.


DM4Cat. No.: HY-12454

DM4 is is an agent that inhibit cellantitubulindivision. DM4 can be used in the preparation ofantibody drug conjugate.


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 0.026 nM.IC50


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.



https://www.MedChemExpress.com/D8-MMAD.html

https://www.MedChemExpress.com/d8-mmae.html

https://www.MedChemExpress.com/D8-MMAF.html

https://www.MedChemExpress.com/D8-MMAF_hydrochloride.html

https://www.MedChemExpress.com/deoxypodophyllotoxin.html

https://www.MedChemExpress.com/dm3.html

https://www.MedChemExpress.com/dm3-sme.html

https://www.MedChemExpress.com/DM4.html

https://www.MedChemExpress.com/dm4-sme.html

https://www.MedChemExpress.com/dm4-spdp.html

Docetaxel (RP-56976) Cat. No.: HY-B0011

Docetaxel is an antineoplastic drug by inhibiting depolymerization, and attenuatingmicrotubule

of the effects of and gene expression.bcl-2 bcl-xL


Docetaxel Trihydrate (RP-56976 (Trihydrate)) Cat. No.: HY-B0011A

Docetaxel Trihydrate is a semi-synthetic taxaneanalogue, acts as a stabilizer.microtubule


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 polymerization.auricularia tubulin

Purity: 98.52%Clinical Data: Phase 2Size: 1 mg, 5 mg

ELR510444Cat. No.: HY-16191

ELR510444 is a novel microtubule disruptor;inhibits MDA-MB-231 cell proliferation with IC50of 30.9 nM; not a substrate for the P-glycoproteindrug transporter and retains activity inβIII-tubulin-overexpressing cell lines.


EntasobulinCat. No.: HY-16777

Entasobulin is a polymerization inhibitorβ-tubulinwith potential anticancer activity.


Epothilone A (Epo A) Cat. No.: HY-13503

Epothilone A is a competitive inhibitor of thebinding of [ H] paclitaxel to polymers,3 tubulinwith a of 0.6-1.4 μM.Ki


Epothilone B (EPO 906; Patupilone) Cat. No.: HY-17029

Epothilone B is a stabilizer with amicrotubule of 0.71μM. It acts by binding to the αβ-tubulinKi

heterodimer subunit which causes decreasing ofαβ-tubulin dissociation.


Epothilone D (KOS 862) Cat. No.: HY-15278

Epothilone D (KOS 862) is a potent microtubulestabilizer.


Eribulin (B1939; E7389; ER-086526) Cat. No.: HY-13442

Eribulin (E7389) is a targetingmicrotubuleagent that is used in the treatment of metastaticbreast cancer. Eribulin (E7389) inhibits theproliferation of cancer cells by bindingmicrotubule proteins and microtubules.

Purity: >98%Clinical Data: LaunchedSize: 1 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 in themicrotubule

treatment of metastatic breast cancer. Eribulinmesylate (E7389 mesylate) inhibits theproliferation of cancer cells by bindingmicrotubule proteins and microtubules.

Purity: 99.52%Clinical Data: LaunchedSize: 500 μg, 1 mg


https://www.MedChemExpress.com/Docetaxel.html

https://www.MedChemExpress.com/docetaxel-trihydrate.html

https://www.MedChemExpress.com/Dolastatin-10.html

https://www.MedChemExpress.com/ELR510444.html

https://www.MedChemExpress.com/Entasobulin.html

https://www.MedChemExpress.com/Epothilone_A.html

https://www.MedChemExpress.com/Epothilone-B.html

https://www.MedChemExpress.com/Epothilone-D.html

https://www.MedChemExpress.com/eribulin.html

https://www.MedChemExpress.com/eribulin-mesylate.html

Estramustine phosphate sodiumCat. No.: HY-13627

Estramustine phosphate sodium is anantimicrotubule chemotherapy agent; arrestsprostate cancer cells in the G2/M phase of thecell cycle.


FlubendazoleCat. No.: HY-B0294

Flubendazole is a safe and efficaciousanthelmintic drug, which is widely used foranthelmintic to human, rodents and ruminants.Flubendazole exerts anticancer activities bymechanisms including inhibition of microtubulefunction.


Fosbretabulin disodium (CA 4DP; CA 4P; Combretastatin A4 disodium phosphate) Cat. No.: HY-17449

Fosbretabulin disodium(CA 4DP; CA 4P) is amicrotubule destabilizing drug, a type ofvascular-targeting agent, a drug designed todamage the vasculature (blood vessels) of cancertumors causing central necrosis.


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: >98%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 50 mg, 100 mg

Ixabepilone (Azaepothilone B; BMS 247550; BMS 247550-1) Cat. No.: HY-10222

Ixabepilone is an orallybioavailable inhibitor,microtubulewhich binds to tubulin and promotes tubulinpolymerization and microtubule stabilization,thereby arrests cells in the G2-M phase of thecell cycle and induces tumor cell apoptosis.


Lexibulin (CYT-997) Cat. No.: HY-10498

Lexibulin(CYT-997) is a potent tubulinpolymerisation inhibitor with IC50 of 10-100 nM incancer cell lines; with potent cytotoxic andvascular disrupting activity in vitro and in vivo.


Lexibulin dihydrochloride (CYT-997 dihydrochloride) Cat. No.: HY-10498A

Lexibulin 2Hcl (CYT-997 2Hcl) is a potent tubulinpolymerisation inhibitor with IC50 of 10-100 nM incancer cell lines; with potent cytotoxic andvascular disrupting activity in vitro and in vivo.


Maytansinol (Ansamitocin P-0) Cat. No.: HY-19474

Maytansinol inhibits microtubule assembly andinduces microtubule disassembly in vitro. Target:Microtubule/Tubulin in vitro: Maytansinol disruptsthe mitotic spindle and prevents mitotic exit inDrosophila.


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: >98%Clinical Data:Size: 100 mg, 250 mg, 500 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.



https://www.MedChemExpress.com/Estramustine-phosphate-sodium.html

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https://www.MedChemExpress.com/fosbretabulin-disodium.html

https://www.MedChemExpress.com/indibulin.html

https://www.MedChemExpress.com/Ixabepilone.html

https://www.MedChemExpress.com/Lexibulin.html

https://www.MedChemExpress.com/Lexibulin-dihydrochloride.html

https://www.MedChemExpress.com/Maytansinol.html

https://www.MedChemExpress.com/mc-alkyl-hydrazine.html

https://www.MedChemExpress.com/Mc-MMAD.html

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.


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.


McMMAF (Maleimidocaproyl monomethylauristatin F) Cat. No.: HY-15578

McMMAF is a protective group-conjugated MMAF. MMAFis a potent tubulin polymerization inhibitor.


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: 98.74%Clinical 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.


Mivobulin (NSC 613862; (S)-(-)-NSC 613862) Cat. No.: HY-106423

Mivobulin (NSC 613862) is a inhibitor,tubulinbinds 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.


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


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.


MMAF Hydrochloride (Monomethylauristatin F Hydrochloride) Cat. No.: HY-15579A

MMAF Hydrochloride (Monomethylauristatin FHydrochloride) is a potent tubulin

inhibitor and is used as apolymerizationantitumor agent.


MMAF sodium (Monomethylauristatin F sodium) Cat. No.: HY-15579B

MMAF sodium (Monomethylauristatin F sodium) is apotent inhibitor and istubulin polymerizationused as a antitumor agent.



https://www.MedChemExpress.com/Mc-MMAE.html

https://www.MedChemExpress.com/mc-val-cit-pab-mmaf.html

https://www.MedChemExpress.com/McMMAF.html

https://www.MedChemExpress.com/Mertansine.html

https://www.MedChemExpress.com/microtubule-inhibitor-1.html

https://www.MedChemExpress.com/mivobulin.html

https://www.MedChemExpress.com/MMAD.html

https://www.MedChemExpress.com/mmaf.html

https://www.MedChemExpress.com/MMAF-Hydrochloride.html

https://www.MedChemExpress.com/mmaf-sodium.html

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 tubulin polymerization.


MPT0B392Cat. No.: HY-101287

MPT0B392, an orally active quinoline derivative,induces activation,c-Jun N-terminal kinase (JNK) leading to .apoptosis


Nocodazole (Oncodazole; R17934) Cat. No.: HY-13520

Nocodazole is a rapidly-reversible inhibitor of. Nocodazole binds to β-tubulin andmicrotubule

disrupts microtubule assembly/disassemblydynamics, which prevents mitosis and inducesapoptosis in tumor cells. Nocodazole inhibits

, and activates .Bcr-Abl CRISPR/Cas9


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.


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.


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.


Paclitaxel (Taxol) Cat. No.: HY-B0015

Paclitaxel (Taxol), a naturally occurringantineoplastic agent, stabilizes tubulin

, resulting in arrest at the G2/Mpolymerizationphase of the cell cycle and apoptotic cell death.


Parbendazole (SKF 29044) Cat. No.: HY-115364

Parbendazole is a potent inhibitor of assembly, destabilizes tubulin,microtubule

with an of 8.79nM, and exhibits aEC50

broad-spectrum anthelmintic activity.


PBOX 6Cat. No.: HY-U00446

PBOX 6 is a pyrrolo-1,5-benzoxazepine (PBOX)compound, acts as a -depolymerizingmicrotubuleagent and an apoptotic agent.


PE859Cat. No.: HY-12662

PE859 is a potent inhibitor of both and tau Aβaggregation with values of 0.66 and 1.2 μM,IC50

respectively.



https://www.MedChemExpress.com/Monomethyl-auristatin-E.html

https://www.MedChemExpress.com/mpt0b392.html

https://www.MedChemExpress.com/Nocodazole.html

https://www.MedChemExpress.com/Ombrabulin.html

https://www.MedChemExpress.com/Ombrabulin-hydrochloride.html

https://www.MedChemExpress.com/OSIP-486823.html

https://www.MedChemExpress.com/Paclitaxel.html

https://www.MedChemExpress.com/Parbendazole.html

https://www.MedChemExpress.com/PBOX_6.html

https://www.MedChemExpress.com/PE859.html

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.


PF-06380101 (Aur0101; Auristatin-0101) Cat. No.: HY-12522

PF-06380101 (Aur0101), an auristatin inhibitor, is a cytotoxicmicrotubule

Dolastatin 10 analogue.


PironetinCat. No.: HY-116446

Pironetin is an α/β unsaturated lactone isolatedfrom species. Pironetin binds toStreptomyces

and is a potent inhibitor ofα-tubulin polymerization, and has cell cyclemicrotubule

arrest and antitumor activity.


Plinabulin (NPI-2358) Cat. No.: HY-14444

Plinabulin (NPI-2358) is a vascular disruptingagen ( ) against withVDA tubulin-depolymerizingan of 9.8 nM against HT-29 cells. PlinabulinIC50

binds the colchicine binding site of β-tubulinpreventing polymerization and has potentinhibitory to tumor cells.


Podofilox (Podophyllotoxin) Cat. No.: HY-15552

Podofilox (Podophyllotoxin) is a potent inhibitorof microtubule assembly and DNA topoisomerase II.


Rosabulin (STA 5312) Cat. No.: HY-14934

Rosabulin is a potent inhibitor,microtubulewith anti-cancer activities.


S516Cat. No.: HY-130233

S516 (Compound 22) is an active metabolite ofCKD-516 and a potent tubulin polymerizationinhibitor with an of 4.29 μM. S516 has markedIC50

antitumor activity.

Purity: >98%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 5 mg, 10 mg, 25 mg, 50 mg, 100 mg

Soblidotin (Auristatin PE; TZT-1027) Cat. No.: HY-14672

Soblidotin (Auristatin PE) is a novel syntheticDolastatin 10 derivative and inhibitor of tubulinpolymerization.

Purity: 99.76%Clinical Data: Phase 2Size: 1 mg, 5 mg, 10 mg, 25 mg, 50 mg

SS28Cat. No.: HY-100761

SS28, a SRT501 analog with oral bioavailability,inhibits to cause celltubulin polymerizationcycle arrest at G2/M phase. SS28 results inapoptosis rather than necrosis tubulin.


SSE15206Cat. No.: HY-111425

SSE15206 is a polymerizationmicrotubuleinhibitor (GI = 197 nM in HCT116 cells) that50

overcomes multidrug resistance. Causes aberrantmitosis resulting in G2/M arrest due to incompletespindle formation in cancer cells.



https://www.MedChemExpress.com/peg4-linker.html


https://www.MedChemExpress.com/pironetin.html

https://www.MedChemExpress.com/plinabulin.html

https://www.MedChemExpress.com/Podophyllotoxin.html

https://www.MedChemExpress.com/Rosabulin.html

https://www.MedChemExpress.com/s516.html

https://www.MedChemExpress.com/Auristatin-PE.html

https://www.MedChemExpress.com/ss28.html

https://www.MedChemExpress.com/SSE15206.html

Taccalonolide ACat. No.: HY-N2416

Taccalonolide A is a microtubule stabilizer, whichis a steroid isolated from , withTacca chantriericytotoxic and antimalarial activities.Taccalonolide A causes G -M accumulation, Bcl-22

phosphorylation and initiation of apoptosis.


Taccalonolide AJCat. No.: HY-N4208

Taccalonolide AJ is a semi-synthesis compound withcellular stabilizing activity.microtubuleTaccalonolide AJ exhibits high potencyantiproliferative activity against cancer cells,with an IC of 4.2 nM for HeLa cells.50


Taccalonolide BCat. No.: HY-N3028

Taccalonolide B is microtubule stabilizer isolatedfrom , with antitumor activity.Tacca plantagineaTaccalonolide B is effective in vitro against celllines that overexpress P-glycoprotein (Pgp) andmultidrug-resistance protein (MRP7).


Taltobulin (HTI-286; SPA-110) Cat. No.: HY-15584

Taltobulin (HTI-286; SPA-110) is an analogue ofHemiasterlin; potent tubulin inhibitor; ADCscytotoxin. IC50 value: Target: tubulin in vitro:HTI-286 significantly inhibited proliferation ofall three hepatic tumor cell lines (mean IC50 = 2nmol/L +/- 1 nmol/L) in vitro.


Taltobulin hydrochloride (HTI-286 hydrochloride; SPA-110 hydrochloride) Cat. No.: HY-15584B

Taltobulin hydrochloride is an analogue ofHemiasterlin; potent tubulin inhibitor; ADCscytotoxin. IC50 value: Target: tubulin in vitro:HTI-286 significantly inhibits proliferation ofall three hepatic tumor cell lines (mean IC50 = 2nmol/L +/- 1 nmol/L).


Taltobulin trifluoroacetate (HTI-286 trifluoroacetate; SPA-110 trifluoroacetate) Cat. No.: HY-15584A

Taltobulin trifluoroacetate (HTI-286; SPA-110) isan analogue of Hemiasterlin; potent tubulininhibitor; ADCs cytotoxin.


Tasidotin hydrochloride (ILX651) Cat. No.: HY-13760

Tasidotin hydrochloride is a peptide analog of theantimitotic depsipeptide dolastatin 15, as aninhibitor of microtubule assembly and microtubuledynamics.


Tirbanibulin (KX2-391; KX-01) Cat. No.: HY-10340

Tirbanibulin (KX2-391) is an inhibitor of Srcthat targets the peptide substrate site of Src,with of 9-60 nM in cancer cell lines.GI50


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 lines.GI50


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.



https://www.MedChemExpress.com/taccalonolide-a.html

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https://www.MedChemExpress.com/taccalonolide-b.html

https://www.MedChemExpress.com/taltobulin.html

https://www.MedChemExpress.com/Taltobulin-hydrochloride.html

https://www.MedChemExpress.com/Taltobulin-trifluoroacetate.html

https://www.MedChemExpress.com/Tasidotin_(hydrochloride).html

https://www.MedChemExpress.com/kx2-391.html

https://www.MedChemExpress.com/KX2-391-dihydrochloride.html

https://www.MedChemExpress.com/KX2-391-Mesylate.html

Triclabendazole (CGA89317) Cat. No.: HY-B0621

Triclabendazole(CGA89317) is a benzimidazole, itbinds to tubulin impairing intracellular transportmechanisms and interferes with protein synthesis.


Tubulin inhibitor 1Cat. No.: HY-112607

Tubulin inhibitor 1 is a inhibitor,tubulininhibits tubulin polymerization. Tubulin inhibitor1 shows potent anti-tumor activity, casuescellular mitotic arrest in the G2/M phase, andinduces cellular .apoptosis


TubulysinCat. No.: HY-128914

Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria

and Archangium geophyra Angiococcus.disciformis


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-angiogenic,and antiproliferative.


Tubulysin BCat. No.: HY-N1243

Tubulysin B is a highly cytotoxic peptide andpotent destabilizing agentsmicrotubuleisolated from the myxobacteria Archangium

and .geophyra Angiococcus disciformis


Tubulysin CCat. No.: HY-N2347

Tubulysin C is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium



Tubulysin DCat. No.: HY-N2348

Tubulysin D is one of the most potent derivativesamong the tubulysins isolated from themyxobacterial species andArchangium geophyra

.Angiococcus disciformis


Tubulysin ECat. No.: HY-N2346

Tubulysin E is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium



Tubulysin FCat. No.: HY-N7049

Tubulysin F is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium



Tubulysin GCat. No.: HY-N7050

Tubulysin G is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium




https://www.MedChemExpress.com/triclabendazole.html

https://www.MedChemExpress.com/Tubulin_inhibitor.html

https://www.MedChemExpress.com/tubulysin.html

https://www.MedChemExpress.com/Tubulysin-A.html

https://www.MedChemExpress.com/tubulysin-b.html

https://www.MedChemExpress.com/tubulysin-c.html

https://www.MedChemExpress.com/tubulysin-d.html

https://www.MedChemExpress.com/tubulysin-e.html

https://www.MedChemExpress.com/tubulysin-f.html

https://www.MedChemExpress.com/tubulysin-g.html

Tubulysin HCat. No.: HY-N7051

Tubulysin H is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium



Tubulysin ICat. No.: HY-N7052

Tubulysin I is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium



Tubulysin MCat. No.: HY-N7053

Tubulysin M is a highly cytotoxic peptide isolatedfrom the myxobacterial species Archangium



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.


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.


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.


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.


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).


VERU-111 (ABI-231) Cat. No.: HY-120599

VERU-111 (ABI-231) is a potent and orallybioavailable inhibitor, whichα and β tubulindisplays strong antiproliferative activity, withan average IC of 5.2 nM against panels of50

melanoma and prostate cancer cell lines.


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.



https://www.MedChemExpress.com/tubulysin-h.html

https://www.MedChemExpress.com/tubulysin-i.html

https://www.MedChemExpress.com/tubulysin-m.html

https://www.MedChemExpress.com/Valecobulin.html

https://www.MedChemExpress.com/valecobulin-hydrochloride.html

https://www.MedChemExpress.com/vat-cit-pab-monomethyl-dolastatin-10.html

https://www.MedChemExpress.com/Vc-MMAD.html

https://www.MedChemExpress.com/VcMMAE.html

https://www.MedChemExpress.com/veru-111.html

https://www.MedChemExpress.com/verubulin.html

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.


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 8.9 μM.IC50


Vincristine (Leurocristine; NSC-67574; 22-Oxovincaleukoblastine) Cat. No.: HY-N0488A

Vincristine (Leurocristine) is amicrotubule-destabilizing agent (MDA). Vincristine(Leurocristine) binds to tubulin and inhibits theformation of microtubules, thereby inhibitingmitosis of the cancer cell.

Purity: >98%Clinical Data: LaunchedSize: 5 mg, 10 mg, 20 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 nM.Ki


Vinorelbine (KW-2307 base) Cat. No.: HY-12053

Vinorelbine is an anti-mitotic agent whichinhibits the proliferation of Hela cells with IC50

of 1.25 nM.

Purity: >98%Clinical 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 1.25 nM.50



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https://www.MedChemExpress.com/vincristine.html

https://www.MedChemExpress.com/vincristine-sulfate.html

https://www.MedChemExpress.com/vinorelbine.html

https://www.MedChemExpress.com/Vinorelbine-ditartrate.html

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.


https://www.MedChemExpress.com/Targets/Mps1.html

Mps1 Inhibitors

AZ3146Cat. No.: HY-14710

AZ3146 is a reasonably potent and selective inhibitor with of 35 nM forMps1 IC50

Mps1 .Cat


BAY1217389Cat. No.: HY-12859

BAY 1217389 is a potent, and selective inhibitorof the monopolar spindle 1 ( ) kinase withMPS1an value less than 10 nM.IC50


BOS-172722Cat. No.: HY-112162

BOS-172722 is an inhibitor of monopolar spindle 1 checkpoint with an of 2 nM.(MPS1) IC50


CCT251455Cat. No.: HY-12603

CCT251455 is a potent and selective mitotic kinasemonopolar spindle 1 ( ) inhibitor with anMPS1

of 3 nM.IC50


Empesertib (BAY 1161909) Cat. No.: HY-12858

Empesertib (BAY 1161909) is a potent Mps1inhibitor, with an of < 1 nM.IC50


MPI-0479605Cat. No.: HY-12660

MPI-0479605 is a potent and selectiveATP-competitive inhibitor of , with an Mps1 IC50

of 1.8 nM.


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 nM.IC50 Kd



Mps1-IN-2 is a potent, selective andATP-competitive dual inhibitor, withMps1/Plk1an and a of 145 nM and 12 nM for Mps1IC50 Kd

and a of 61 nM for Plk1.Kd



Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor, with an of 50 nM.IC50


NMS-P715Cat. No.: HY-12382

NMS-P715 is a selective, ATP-competitive inhibitorof , with an of 182 nM.MPS1 IC50

Purity: >99.0%Clinical Data: No Development ReportedSize: 5 mg, 10 mg, 50 mg, 100 mg


https://www.MedChemExpress.com/Targets/Mps1.html

https://www.MedChemExpress.com/AZ3146.html

https://www.MedChemExpress.com/BAY1217389.html

https://www.MedChemExpress.com/BOS-172722.html

https://www.MedChemExpress.com/CCT251455.html

https://www.MedChemExpress.com/BAY-1161909.html

https://www.MedChemExpress.com/MPI-0479605.html

https://www.MedChemExpress.com/Mps1-IN-1.html

https://www.MedChemExpress.com/Mps1-IN-2.html

https://www.MedChemExpress.com/mps1-in-3.html

https://www.MedChemExpress.com/NMS-P715.html

TC-Mps1-12Cat. No.: HY-110115

TC-Mps1-12 is a potent and selective monopolar inhibitor, with an of 6.4spindle 1 (Mps1) IC50

nM.



https://www.MedChemExpress.com/tc-mps1-12.html

Myosin

Myosin light chain kinase (MLCK) is a ubiquitous Ca /calmodulin (CaM)-activated kinase found in smooth, cardiac, and skeletal2+

muscle as well as in mammalian nonmuscle cells.

Myosin light chain kinase (MLCK) is a regulatory protein forsmooth muscle contraction, which acts by phosphorylating20-kDamyosin light chain (MLC20) to activate the myosin ATPase activity.Myosin light chain kinase (MLCK) of smooth musclehasbeen puried as an enzyme that phosphorylates 20-kDa lightchain of smoothmuscle myosin (MLC20).

Analysis of the cross talk between Ras-ERK and PI3K-AKT signaling pathways reveals integrin β1, myosin light chain kinase (MLCK)and myosin IIA are required for the activation of PI3K-AKT following inhibition of the Ras-ERK pathway. Integrin β1, MLCK, andmyosin IIA are factors in the development of resistance to MEK inhibitors.

Myosin light chain kinase (MLCK) phosphorylates the regulatory light chain (RLC) of myosin producing increases in forcedevelopment during skeletal muscle contraction.


https://www.MedChemExpress.com/Targets/Myosin.html

Myosin Inhibitors, Activators & Modulators

(-)-Blebbistatin ((S)-(-)-Blebbistatin) Cat. No.: HY-13441

(-)-Blebbistatin is an S enantiomer ofblebbistatin. Blebbistatin is a potent andselective inhibitor with s rangingmyosin II IC50

from 0.5 to 5 μM.


ATM-3507Cat. No.: HY-100948

ATM-3507 is a potent inhibitor withtropomyosins from 3.83-6.84 μM in human melanoma cellIC50

lines.


ATM-3507 trihydrochlorideCat. No.: HY-100948B

ATM-3507 trihydrochloride is a potent inhibitor with s from 3.83-6.84tropomyosin IC50

μM in human melanoma cell lines.


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: >97.0%Clinical Data: No Development ReportedSize: 1 mg

BTS (N-Benzyl-p-toluenesulfonamide; N-Tosylbenzylamine) Cat. No.: HY-16690

BTS is a potent inhibitor of Ca2+-stimulatedmyosin S1 ATPase (IC50 ~ 5 μM) and reversiblyblocks the gliding motility.

Purity: 99.78%Clinical Data: No Development ReportedSize: 10 mM × 1 mL, 500 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, respectively.IC50


Mavacamten (MYK461; SAR439152) Cat. No.: HY-109037

Mavacamten is a modulator of ,cardiac myosinwith of 490, 711 nM for bovine cardiac andIC s50

human cardiac, respectively.


ML-7 hydrochlorideCat. No.: HY-15417

ML-7 hydrochloride is a naphthalene sulphonamidederivative, potently inhibits ( =300MLCK IC50

nM).


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 μM,Ki

respectively.


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.



https://www.MedChemExpress.com/Targets/Myosin.html

https://www.MedChemExpress.com/_-_-Blebbistatin.html

https://www.MedChemExpress.com/ATM-3507.html

https://www.MedChemExpress.com/atm-3507-trihydrochloride.html

https://www.MedChemExpress.com/blebbistatin.html

https://www.MedChemExpress.com/BTS.html

https://www.MedChemExpress.com/HA-100.html

https://www.MedChemExpress.com/Mavacamten.html

https://www.MedChemExpress.com/ML-7-hydrochloride.html

https://www.MedChemExpress.com/ml-9.html

https://www.MedChemExpress.com/ml-9-free-base.html

MLCK inhibitor peptide 18Cat. No.: HY-P1029

MLCK inhibitor peptide 18 is a myosin light chainkinase ( ) inhibitor with an of 50 nM,MLCK IC50

and inhibits only at 4000-foldCaM kinase IIhigher concentrations.

Purity: 98.71%Clinical 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 μM.IC50


Omecamtiv mecarbil (CK-1827452) Cat. No.: HY-14233

Omecamtiv mecarbil is a selective cardiac myosinactivator.


para-NitroblebbistatinCat. No.: HY-120870

para-Nitroblebbistatin is a non-cytotoxic,photostable, fluorescent and specific Myosin IIinhibitor, usd in the study of the specific roleof myosin II in physiological, developmental, andcell biological studies.



https://www.MedChemExpress.com/MLCK_inhibitor_peptide_18.html

https://www.MedChemExpress.com/MS-444.html

https://www.MedChemExpress.com/Omecamtiv-mecarbil.html

https://www.MedChemExpress.com/para-nitroblebbistatin.html

PAKp21 activated kinases

PAKs (p21-activated kinases) are key regulators of actin dynamics, cell proliferation and cell survival. PAKs are Ser/Thr kinases thatare classified into two groups on the basis of their structural and functional features: group I (PAK1–3) and group II (PAK4–6). 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 diseases,small-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, invasion,migration and regulation of cell cycle and mitosis. Consequently, PAKs have also been implicated in a number of pathologicalconditions including cancer.


https://www.MedChemExpress.com/Targets/PAK.html

PAK Inhibitors & 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: >98.0%Clinical Data: LaunchedSize: 10 mM × 1 mL, 500 mg, 10 g

Fingolimod (FTY720 free base) Cat. No.: HY-11063

Fingolimod is a ( )sphingosine 1-phosphate S1Pantagonist with of 0.033 nM in K562 and NKIC50

cells. Fingolimod also is a activator, apak1immunosuppressant.


Fingolimod hydrochloride (FTY720) Cat. No.: HY-12005

Fingolimod hydrochloride is a sphingosine ( ) antagonist with an of1-phosphate S1P IC50

0.033 nM in K562 and NK cells. Fingolimodhydrochloride also is a activator.pak1

Purity: 99.86%Clinical Data: LaunchedSize: 10 mM × 1 mL, 100 mg, 200 mg, 1 g, 5 g

FRAX1036Cat. No.: HY-19538

FRAX1036 is a inhibitor with s of 23.3 nM,PAK Ki

72.4 nM, and 2.4 μM for PAK1, PAK2 and PAK4,respectively.


FRAX486Cat. No.: HY-15542B

FRAX486 is a p21-activated kinase ( ) inhibitorPAKwith s of 14, 33 and 39 nM for PAK1, PAK2 andIC50

PAK3, respectively.


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


G-5555Cat. No.: HY-19635

G-5555 is a potent p21-activated kinase 1 ( )PAK1inhibitor with s of 3.7 nM and 11 nM for PAK1Ki

and PAK2, respectively.


G-5555 hydrochlorideCat. No.: HY-19635A

G-5555 hydrochloride is a potent and selectivep21-activated kinase 1 ( ) inhibitor with a PAK1 Ki

of 3.7 nM.


GNE 2861Cat. No.: HY-12632

GNE 2861 is a inhibitor that displays groupPAKII selectivity. GNE 2861 inhibits PAK4, PAK5 andPAK6 with s of 7.5, 36, 126 nM, respectively.IC50


IPA-3Cat. No.: HY-15663

IPA-3 is a selective non-ATP competitive PAK1inhibitor with of 2.5 μM, and shows noIC50

inhibition to group II PAKs (PAKs 4-6).



https://www.MedChemExpress.com/Targets/PAK.html

https://www.MedChemExpress.com/5-Aminosalicylic-acid.html

https://www.MedChemExpress.com/fingolimod.html

https://www.MedChemExpress.com/Fingolimod-hydrochloride.html

https://www.MedChemExpress.com/FRAX1036.html



https://www.MedChemExpress.com/G-5555.html

https://www.MedChemExpress.com/G-5555_hydrochloride.html

https://www.MedChemExpress.com/PAK-IN-1.html

https://www.MedChemExpress.com/IPA-3.html

NVS-PAK1-1Cat. No.: HY-100519

NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nM.PAK1 IC50


PF-3758309Cat. No.: HY-13007

PF-3758309 is a potent, orally available, andreversible ATP-competitive inhibitor of PAK4( = 2.7 nM; =18.7 nM).Kd Ki



https://www.MedChemExpress.com/NVS-PAK1-1.html


Cytoskeleton - MedchemExpress.com...Inhibitors, Agonists, Screening Libraries Cytoskeleton The...

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