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You are here:Home-Inhibitors & Agonists-Cytoskeleton/Cell Adhesion Molecules-Kinesin

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Kinesin is a protein belonging to a class of motor proteins found in eukaryotic cells. Kinesins move along microtubule filaments, and are powered by the hydrolysis of ATP (thus kinesins are ATPases). The active movement of kinesins supports several cellular functions including mitosis, meiosis and transport of cellular cargo. Most kinesins walk towards the plus end of a microtubule, entails transporting cargo from the centre of the cell towards the periphery. Kinesins were discovered as microtubule (MT)-based anterograde intracellular transport motors. The founding member of this superfamily, the genomes of mammals encode more than 40 kinesin proteins, organized into at least 14 families named kinesin-1 through kinesin-14.

Cat. No. Product Name CAS No. Information
GY10361

GW406108X

1644443-92-4

GW406108X (GW-406108X, GW108X) is specific inhibitor of Kif15 (Kinesin-12) with IC50 of 0.82 uM in ATPase assays; GW108X displays a preference for Kif15 over the other mitotic motors, with 30 ¦ÌM of GW108X inhibiting Kif15 MT gliding by 98.9% ¡À 0.2% while only inhibiting Eg5 by 19.8% ¡À 4.3%, HSET by 5.3% ¡À 2.9% and Kif18A by 4.9%; inhibits the MT-stimulated ATPase and MT gliding activity of Kif15 either by inhibiting ATP binding or by inhibiting MT binding by the motorl; shows a distinct mechanism of action compared with the Kif15 inhibitor, Kif15-IN-1.

GY02138

GSK-923295

1088965-37-0

Benzamide, 3-chloro-N-[(1S)-2-[[2-(dimethylamino)acetyl]amino]-1-[[4-[8-[(1S)-1-hydroxyethyl]imidazo[1,2-a]pyridin-2-yl]phenyl]methyl]ethyl]-4-(1-methylethoxy)-

GY02025

PF-2771

PF-2771 is a potent, selective CENP-E inhibitor with IC50 of 16.1 nM; does not inhibit the ATPase activities of highly related kinesins (Eg5/KSP, chromokinesin and MCAK, IC50> 1 uM); selectively inhibits proliferation of basal breast cancer cell lines; regresses tumor growth correlated with increased phospho-HH3-Ser10 levels in a breast cancer xenograft tumor model.

GY03611

Dimethylenastron

863774-58-7

A small molecule inhibitor of the mitotic kinesin Eg5; inhibits endothelial cell proliferation and migration in vitro; exhibits a shorter mitotic arrest, bipolar or multipolar karyokinesis, followed by apoptosis of the daughter cells in dimethylenastron-treated tetraploid cells.

GY03511

K858

72926-24-0

A potent, selective inhibitor of mitotic kinesin Eg5 ATPase activity with IC50 of 1.3 uM; displays >150-fold more selective for Eg5 than other members of the kinesin superfamily; induces mitotic arrest, apoptosis, and cell growth inhibition through the activation of the Mad2-mediated spindle checkpoint, and has no effect on microtubule polymerization; exhibits potent antitumor activity in xenograft models of cancer, and induces the accumulation of mitotic cells with monopolar spindles in tumor tissues.

GY03474

Kif15-IN-1

672926-32-8

Kif15-IN-1 is a potent, selective inhibitor of KIF15 motility, can act synergistically with Eg5 inhibitors to impair cancer cell proliferation.

GY03173

Monastrol

329689-23-8

Monastrol is a potent, specific, allosteric and reversible mitotic kinesin Eg5 inhibitor with IC50 of 14 uM (microtubule motility inhibition); does not inhibit microtubule motility driven by conventional kinesin at 200 uM; inhibits both the basal and the microtubule-stimulated ATPase activity of the Eg5 motor domain, does not compete with ATP binding to Eg5; arrests cells in mitosis with monoastral spindles, and (S)-monastrol is a more potent inhibitor of Eg5 activity in vitro and in vivo.

GY01622

SB-743921

940929-33-9

SB-743921 is a potent, selective kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, shows no activity against MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E; also shows high affinity for mouse KSP with Ki of 0.12 nM; blocks assembly of a functional mitotic spindle, thereby causing cell cycle arrest in mitosis and subsequent cell death in cancer cells, demonstrates improved potency over ispinesib in both biochemical and cellular assays; shows a broad spectrum of tumor inhibition in multiple cancer models.

GY01315

Ispinesib

336113-53-2

Ispinesib is a potent, selective, cell-permeable, allosteric inhibitor of Eg5 (mitotic kinesin KSP) with Ki of 2.3 nM; displays >10,000-fold selectivity for Eg5 over a range of other mitotic kinesins; induces a monopolar spindle phenotype, leading to the activation of a spindle assembly checkpoint, mitotic arrest, and subsequent cell death with GI50 of 20-80 nM in colon, pancreas, prostrate, and lung cancer cells; demonstrates tumor regression of breast cancer cell xenografts in mice at 10 mg/kg.

GY06084

MK-8267

1146209-50-8

MK-8267 (SCH 2047069) is a potent, orally bioavailable, brain penetrant kinesin spindle protein (KSP) inhibitor with EC50 of 3 nM; inhibits a broader panel of 57 different tumor cell lines with IC50 <30 nM; showes significant brain uptake in mouse and rat with brain/plasma AUC ratio of 4 in rats, demonstrates anti-tumor activities in the tumor xenograft mouse model.

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