| 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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