Cytoskeleton - file.medchemexpress.comfile.medchemexpress.com/pathwayPDF/Cytoskeleton... · Cytoskeleton The cytoskeleton is a filamentous network of F-actin, microtubules, and intermediate

Inhibitors Agonists Screening LibrarieswwwMedChemExpresscom

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

wwwMedChemExpresscom 1

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


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


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)


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



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


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


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


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



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


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


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


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


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


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


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



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


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


AT-1002 TFACat No HY-114426A

AT-1002 TFA a 6-mer synthetic peptide is a tight regulator and absorption enhancerjunction


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



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


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 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)


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


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


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


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


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


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


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


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


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


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


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



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


CarotegrastCat No HY-14857

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

activities


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


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


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


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 02 08 15 and 18 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 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



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


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


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 (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


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


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


EptifibatideCat No HY-B0686

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

with anti-plateletglycoprotein IIbIIIa receptoractivity


Eptifibatide acetateCat No HY-B0686A

Eptifibatide acetate is a cyclic heptapeptideacts as a competitive antagonist for the activatedplatelet withglycoprotein IIbIIIa receptoranti-platelet activity


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



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


GLPG0187Cat No HY-100506

GLPG0187 is a broad spectrum receptorintegrinantagonist with antitumor activity inhibitsα β -integrin with an of 13 nMv 1 IC50


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


GRGDSPCat No HY-P0290

GRGDSP a synthetic linear RGD peptide is an inhibitorintegrin


GRGDSP TFACat No HY-P0290A

GRGDSP (TFA) is an inhibitorintegrin


HSDVHK-NH2Cat No HY-P1187

HSDVHK-NH2 is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50

pgmL (2414 pM)ltbrgt


HSDVHK-NH2 TFACat No HY-P1187A

HSDVHK-NH2 TFA is an antagonist of the integrin interaction with an of 174αvβ3-vitronectin IC50



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


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

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



ILK-IN-3Cat No HY-115677

ILK-IN-3 is an inhibitor withintegrin linked kinaseantitumor activity


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 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


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


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


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


LDVCat No HY-P2267

LDV a non-fluorescent derivative of LDV FITC isa ligand (K ~ 12 nM)α4β1 integrin (VLA-4) d


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


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



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


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


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)


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


RGDCat No HY-P0278

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


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


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


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


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


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


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


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


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


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


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



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


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


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 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


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



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


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


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


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


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 nMIC50


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


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


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


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



Ispinesib (SB-715992) Cat No HY-50759

Ispinesib is a specific inhibitor of kinesin with a of 17 nMspindle protein (KSP) Ki app


K858 (Racemic)Cat No HY-19966

K858 Racemic is an ATP-uncompetitive inhibitor of with an of 13 μMkinesin Eg5 IC50


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-2 is an inhibitor of the mitotic kinesin and is used for the research of cellularKif15

proliferative diseases


Litronesib (LY2523355) Cat No HY-14846

Litronesib (LY2523355) is a selectivemitosis-specific inhibitor withkinesin Eg5antitumor activity


Litronesib Racemate (LY2523355 Racemate) Cat No HY-14846A

Litronesib Racemate (LY2523355 Racemate) is theracemate of litronesib Litronesib is a selectiveallosteric inhibitor of kinesin Eg5


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


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


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


SB-743921Cat No HY-12069

SB-743921 is a potent inhibitor of the mitotic with a of 01 nMkinesin KSP (Eg5) Ki



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


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


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


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)


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


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 15 and 34 μM in neuroblastomaand non-neuroblastoma cell lines respectively



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 13 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)

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


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


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)


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


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


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


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


BTB-1Cat No HY-101770

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

of 169 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


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 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


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


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


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


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


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



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


CurvulinCat No HY-119692

Curvulin isolated from is aCurvularia lunataphytotoxin Curvularin is reported to inhibit

assembly and has also been shown tomicrotubuleinhibit iNOS expression


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


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


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


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)


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-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


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


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


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


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



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 polymers3 tubulinwith a of 06-14 μMKi


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


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 for the research of metastaticbreast cancer Eribulin inhibits the proliferationof cancer cells by binding microtubule proteinsand microtubules


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


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


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


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

Fosbretabulin disodium (CA 4DP) is a tubulindestabilizing agent



Indibulin (ZIO 301 D 24851) Cat No HY-13649

Indibulin (ZIO 301) an orally applicableinhibitor of assembly shows potenttubulinanticancer activity with a minimal neurotoxicity


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


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


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


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


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


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


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


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 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


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


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 (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


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

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


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



MyoseverinCat No HY-W008956

Myoseverina a microtubule-binding moleculeinduces the reversible fission of multinucleatedmyotubes into mononucleated fragments


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


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


PaclitaxelCat No HY-B0015

Paclitaxel is a naturally occurring antineoplasticagent and stabilizes polymerizationtubulinPaclitaxel can cause both mitotic arrest and

cell death Paclitaxel also inducesapoptoticautophagy


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


PBOX 6Cat No HY-U00446

PBOX 6 is a pyrrolo-15-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 066 and 12 μMIC50

respectively


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


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


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


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


Podofilox (Podophyllotoxin) Cat No HY-15552

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


PodophyllotoxoneCat No HY-N2415

Podophyllotoxone is isolated from the roots of and has anti-cancerDysosma versipellis

activitiesPodophyllotoxone is able to inhibit the polymerizationtubulin


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


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


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


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


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


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


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


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


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


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)


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


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


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



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



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


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


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


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 inhibitortubulininhibits tubulin polymerization Tubulin inhibitor1 shows potent anti-tumor activity casuescellular mitotic arrest in the G2M phase andinduces cellular apoptosis



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



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







TubulysinCat No HY-128914

Tubulysin family of secondary metabolites areoriginally isolated from the myxobacteria

and Archangium geophyra Angiococcusdisciformis


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



Tubulysin CCat No HY-N2347

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

and geophyra Angiococcus disciformis


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



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 IM-2Cat No HY-130959

Tubulysin IM-2 is an and tubulinADC Cytotoxinbinder used as anti-microtubule toxins





Tubulysin MCat No HY-N7053

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


Purity gt98Clinical DataSize 25 mg 50 mg 100 mg


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)

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


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 89 μMIC50


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



VindolineCat No HY-N0687

Vindoline a vinca alkaloid extracted from theleaves of weakly inhibitsCatharanthus roseustubulin self-assembly


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


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



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


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 nMIC50


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


CCT251455Cat No HY-12603

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

of 3 nMIC50


Empesertib (BAY 1161909) Cat No HY-12858

Empesertib (BAY 1161909) is a potent Mps1inhibitor with an of lt 1 nMIC50


MPI-0479605Cat No HY-12660

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

of 18 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 nMIC50 Kd


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



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



Mps1-IN-3 is a potent and selective kinaseMPS1inhibitor with an of 50 nMIC50



NMS-P715Cat No HY-12382

NMS-P715 is a selective ATP-competitive inhibitorof with an of 182 nMMPS1 IC50


TC-Mps1-12Cat No HY-110115

TC-Mps1-12 is a potent and selective monopolar inhibitor with an of 64spindle 1 (Mps1) IC50

nM



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


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


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

(-)-Blebbistatin is a selective inhibitor of theATPase activity of non-muscle myosin II


ATM-3507Cat No HY-100948

ATM-3507 is a potent inhibitor withtropomyosins from 383-684 μM in human melanoma cellIC50

lines


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


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


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


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


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


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


ML-7 hydrochlorideCat No HY-15417

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

nM) ML-7 hydrochloride also inhibits YAPTAZ



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


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


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


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


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-cytotoxicphotostable fluorescent and specific Myosin IIinhibitor usd in the study of the specific roleof myosin II in physiological developmental andcell biological studies


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



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


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


FRAX1036Cat No HY-19538

FRAX1036 is a inhibitor with s of 233 nMPAK Ki

724 nM and 24 μM for PAK1 PAK2 and PAK4respectively


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 37 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 37 nM


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


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)



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


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


NVS-PAK1-1Cat No HY-100519

NVS-PAK1-1 is a potent and selective allosteric inhibitor with an of 5 nMPAK1 IC50


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


PF-3758309Cat No HY-13007

PF-3758309 is a potent orally available andreversible ATP-competitive inhibitor of PAK4( = 27 nM =187 nM)Kd Ki


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



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


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


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


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


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


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


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


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


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


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


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



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


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


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


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



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


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


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


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



GSK429286A is a selective inhibitor of withROCK1an value of 14 nMIC50


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



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


Hydroxyfasudil (HA-1100) Cat No HY-13911

Hydroxyfasudil is a inhibitor with s ofROCK IC50

073 and 072 μM for and ROCK1 ROCK2respectively


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


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


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


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


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


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



ROCK-IN-1Cat No HY-U00351

ROCK-IN-1 is a potent inhibitor of with anROCK of 12 nM for ROCK2IC50


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


ROCK2-IN-2Cat No HY-103620

ROCK2-IN-2 is a selective inhibitorROCK2extracted from patent US20180093978A1 CompoundA-30 has an of lt1 μMIC50


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


SAR407899 hydrochlorideCat No HY-15687

SAR407899 hydrochloride is a selective potent andATP-competitive inhibitor with an ofROCK IC50



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


SR-3677Cat No HY-13300

SR-3677 is a potent and selective inhibitorROCK-IIwith an of ~3 nMIC50


ThiazovivinCat No HY-13257

Thiazovivin is a potent inhibitor which canROCKprotect human embryonic stem cells Thiazovivinimproves the efficiency of iPSC generation


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


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



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


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



Y-33075 dihydrochloride is a selective ROCKinhibitor with an of 36 nMIC50


ZINC00881524Cat No HY-101244

ZINC00881524 is a inhibitorROCK



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


Target List in Cytoskeleton




















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
























nM








Dynamin



Dynamin Inhibitors






receptors






























AT-1002Cat No HY-114426






















































Integrin






A-205804Cat No HY-100226















BI-1950Cat No HY-124040




































activities











































of 20 nM


E7820 (ER68203-00) Cat No HY-14571























148 nM







and 65 μM





and 65 μM


















5 nM respectively















of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244






















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
























nM








Dynamin



Dynamin Inhibitors






receptors






























AT-1002Cat No HY-114426






















































Integrin






A-205804Cat No HY-100226















BI-1950Cat No HY-124040




































activities











































of 20 nM


E7820 (ER68203-00) Cat No HY-14571























148 nM







and 65 μM





and 65 μM


















5 nM respectively















of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244

















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
























nM








Dynamin



Dynamin Inhibitors






receptors






























AT-1002Cat No HY-114426






















































Integrin






A-205804Cat No HY-100226















BI-1950Cat No HY-124040




































activities











































of 20 nM


E7820 (ER68203-00) Cat No HY-14571























148 nM







and 65 μM





and 65 μM


















5 nM respectively















of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244









Dynamin



Dynamin Inhibitors






receptors






























AT-1002Cat No HY-114426






















































Integrin






A-205804Cat No HY-100226















BI-1950Cat No HY-124040




































activities











































of 20 nM


E7820 (ER68203-00) Cat No HY-14571























148 nM







and 65 μM





and 65 μM


















5 nM respectively















of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244




Dynamin



Dynamin Inhibitors






receptors






























AT-1002Cat No HY-114426






















































Integrin






A-205804Cat No HY-100226















BI-1950Cat No HY-124040




































activities











































of 20 nM


E7820 (ER68203-00) Cat No HY-14571























148 nM







and 65 μM





and 65 μM


















5 nM respectively















of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244




Dynamin Inhibitors






receptors






























AT-1002Cat No HY-114426






















































Integrin






A-205804Cat No HY-100226















BI-1950Cat No HY-124040




































activities











































of 20 nM


E7820 (ER68203-00) Cat No HY-14571























148 nM







and 65 μM





and 65 μM


















5 nM respectively















of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244









AT-1002Cat No HY-114426






















































Integrin






A-205804Cat No HY-100226















BI-1950Cat No HY-124040




































activities











































of 20 nM


E7820 (ER68203-00) Cat No HY-14571























148 nM







and 65 μM





and 65 μM


















5 nM respectively















of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244





AT-1002Cat No HY-114426






















































Integrin






A-205804Cat No HY-100226















BI-1950Cat No HY-124040




































activities











































of 20 nM


E7820 (ER68203-00) Cat No HY-14571























148 nM







and 65 μM





and 65 μM


















5 nM respectively















of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244

























Integrin






A-205804Cat No HY-100226















BI-1950Cat No HY-124040




































activities











































of 20 nM


E7820 (ER68203-00) Cat No HY-14571























148 nM







and 65 μM





and 65 μM


















5 nM respectively















of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244




Integrin






A-205804Cat No HY-100226















BI-1950Cat No HY-124040




































activities











































of 20 nM


E7820 (ER68203-00) Cat No HY-14571























148 nM







and 65 μM





and 65 μM


















5 nM respectively















of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244





A-205804Cat No HY-100226















BI-1950Cat No HY-124040




































activities











































of 20 nM


E7820 (ER68203-00) Cat No HY-14571























148 nM







and 65 μM





and 65 μM


















5 nM respectively















of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244












activities











































of 20 nM


E7820 (ER68203-00) Cat No HY-14571























148 nM







and 65 μM





and 65 μM


















5 nM respectively















of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244
















of 20 nM


E7820 (ER68203-00) Cat No HY-14571























148 nM







and 65 μM





and 65 μM


















5 nM respectively















of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244






148 nM







and 65 μM





and 65 μM


















5 nM respectively















of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244













of 129 nMEC50













LDVCat No HY-P2267









LXW7Cat No HY-P0178











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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244









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














RGDCat No HY-P0278


















SB-267268Cat No HY-19306




















αvβ3












TR-14035Cat No HY-15770






































Kinesin




Kinesin Inhibitors








AZ82Cat No HY-12241






75 μM




















GW406108X (GW108X) Cat No HY-115570



of 637 (427 nM)pIC50

























14 μM












SB-743921Cat No HY-12069




MicrotubuleTubulin










Zuccwallichiana
























ABT-751 (E7010) Cat No HY-13270











































of 169 μM




















tumor cell line





tumor cell line





of 3 nM



















D-64131Cat No HY-15482






























DM4Cat No HY-12454
































ENMD-1198 (IRC-110160) Cat No HY-16196

































supgt


















































cells























































respectively






































antitumor activity











































of 07 microM












cancer cell lines



















































































































of 125 nM










Mps1 Inhibitors



Mps1 Cat





BOS-172722Cat No HY-112162






of 3 nMIC50





MPI-0479605Cat No HY-12660


of 18 nM






















nM



Myosin
















lines













2+






















respectively









MS-444 (BE-34776) Cat No HY-100685


value of 10 μMIC50



































PAK3 respectively




and PAK1 2 3


G-5555Cat No HY-19635






of 37 nM













apoptosis













PF-3758309Cat No HY-13007































CCG-222740Cat No HY-121750















respectively





respectively





respectively















respectively











GSK269962A (GSK 269962) Cat No HY-15556




























respectivelyROCK2















respectivelyROCK1








62 nM respectively




respectively

























ROCK2 respevtively












Y-27632Cat No HY-10071









Y-33075 (Y 39983) Cat No HY-10067






ZINC00881524Cat No HY-101244




Cytoskeleton - file.medchemexpress.comfile.medchemexpress.com/pathwayPDF/Cytoskeleton... · Cytoskeleton The cytoskeleton is a filamentous network of F-actin, microtubules, and intermediate

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