Kinesin
Inhibitory Selectivity
Isoform-specific Inhibitors
Kinesin Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7090 |
GSK923295GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183. GSK923295 induces post-mitotic apoptosis. Phase 1. |
(f) HeLa cells were treated with mitotic kinesin CENP-E inhibitor GSK923295 (50 nM) for 1 h to generate misaligned kinetochores. After fixation, cells were stained for ACA, tubulin, and TIP60. Statistical significance was tested by two-sided t-test and represented by asterisks corresponding to ***, p < 0.001. Scale bars, 5 μm. |
|
| S0279 |
DimethylenastronDimethylenastron is a potent, specific and reversible inhibitor of kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) with IC50 of 200 nM. Dimethylenastron induces mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells. |
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| S6953New |
GW406108XGW406108X (GW108X) is an inhibitor of Kif15 (Kinesin-12) with an IC50 of 0.82 μM in the ATPase assay. GW406108X inhibits recombinant ULK1 kinase activity with a pIC50 of 6.37 and blocks autophagy in cells, without affecting the upstream signalling kinases mTORC1 and AMPK. |
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| S8439 |
MonastrolMonastrol ((±)-Monastrol) is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) which is essential for maintaining separation of the half-spindles. |
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| S5522 |
H-Cys(Trt)-OHH-Cys(Trt)-OH (L-Cys(Trt)-OH, H-L-Cys(Trt)-OH, S-Tritylcysteine) is a specific inhibitor of Eg5 that inhibits Eg5-driven microtubule sliding velocity in a reversible fashion with an IC50 of 500 nM. |
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| S5933 |
K 858K858 is a novel and potent inhibitor of Eg5 with an IC50 of 1.3 μM for inhibiting the ATPase activity of Eg5, showing at least 150-fold more selective for Eg5 than other members of the kinesin superfamily. |
||
| S6796 |
BTB-1BTB-1 is a novel, selective and reversible inhibitor of the mitotic motor protein Kif18A with IC50 of 1.69 μM. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S7090 |
GSK923295GSK923295 is a first-in-class, specific allosteric inhibitor of CENP-E kinesin motor ATPase with Ki of 3.2 nM, and less potent to mutant I182 and T183. GSK923295 induces post-mitotic apoptosis. Phase 1. |
(f) HeLa cells were treated with mitotic kinesin CENP-E inhibitor GSK923295 (50 nM) for 1 h to generate misaligned kinetochores. After fixation, cells were stained for ACA, tubulin, and TIP60. Statistical significance was tested by two-sided t-test and represented by asterisks corresponding to ***, p < 0.001. Scale bars, 5 μm. |
|
| S0279 |
DimethylenastronDimethylenastron is a potent, specific and reversible inhibitor of kinesin Eg5 (kinesin-5/kinesin spindle protein, KSP) with IC50 of 200 nM. Dimethylenastron induces mitotic arrest and apoptosis and upregulate Hsp70 in human multiple myeloma cells. |
||
| S6953New |
GW406108XGW406108X (GW108X) is an inhibitor of Kif15 (Kinesin-12) with an IC50 of 0.82 μM in the ATPase assay. GW406108X inhibits recombinant ULK1 kinase activity with a pIC50 of 6.37 and blocks autophagy in cells, without affecting the upstream signalling kinases mTORC1 and AMPK. |
||
| S8439 |
MonastrolMonastrol ((±)-Monastrol) is a cell-permeable small molecule inhibitor of kinesin-5(KIF11) which is essential for maintaining separation of the half-spindles. |
||
| S5522 |
H-Cys(Trt)-OHH-Cys(Trt)-OH (L-Cys(Trt)-OH, H-L-Cys(Trt)-OH, S-Tritylcysteine) is a specific inhibitor of Eg5 that inhibits Eg5-driven microtubule sliding velocity in a reversible fashion with an IC50 of 500 nM. |
||
| S5933 |
K 858K858 is a novel and potent inhibitor of Eg5 with an IC50 of 1.3 μM for inhibiting the ATPase activity of Eg5, showing at least 150-fold more selective for Eg5 than other members of the kinesin superfamily. |
||
| S6796 |
BTB-1BTB-1 is a novel, selective and reversible inhibitor of the mitotic motor protein Kif18A with IC50 of 1.69 μM. |
