Kinesin
Signaling Pathway Map
Research Area
Inhibitory Selectivity
Kinesin Products
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1452 |
Ispinesib (SB-715992)Ispinesib (SB-715992, CK0238273) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP) with Ki app of 1.7 nM in a cell-free assay, no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Ispinesib induces mitotic arrest and apoptotic cell death. Phase 2. |
Representative photographs of fluorescent staining of microtubules and nuclei in MDA-MB-231 cells 24 h post-treatment with 4 nM of ispinesib or vinblastine or their combination. Arrows and arrowheads denote mitotic cells with monoploar and bipolar spindles, respectively. Scale bars, 20 um.
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| S2182 |
SB743921 HClSB743921 is a kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, almost no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E. Phase 1/2. |
HeLa cells expressing iRFP were seeded onto 96-well plates and incubated with buffer or different concentrations of SB743921.During the next five days, the plate was scanned with an infrared imaging system (upper panel) to quantify the infrared signals (lower panel). |
|
| 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. |
|
| S7355 |
ARQ 621ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1. |
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| S0279New |
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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| S6796New |
BTB-1BTB-1 is a novel, selective and reversible inhibitor of the mitotic motor protein Kif18A with IC50 of 1.69 μM. |
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| S8439 |
MonastrolMonastrol 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. |
| Catalog No. | Information | Product Use Citations | Product Validations |
|---|---|---|---|
| S1452 |
Ispinesib (SB-715992)Ispinesib (SB-715992, CK0238273) is a potent, specific and reversible inhibitor of kinesin spindle protein (KSP) with Ki app of 1.7 nM in a cell-free assay, no inhibition to CENP-E, RabK6, MCAK, MKLP1, KHC or Kif1A. Ispinesib induces mitotic arrest and apoptotic cell death. Phase 2. |
Representative photographs of fluorescent staining of microtubules and nuclei in MDA-MB-231 cells 24 h post-treatment with 4 nM of ispinesib or vinblastine or their combination. Arrows and arrowheads denote mitotic cells with monoploar and bipolar spindles, respectively. Scale bars, 20 um.
|
|
| S2182 |
SB743921 HClSB743921 is a kinesin spindle protein (KSP) inhibitor with Ki of 0.1 nM, almost no affinity to MKLP1, Kin2, Kif1A, Kif15, KHC, Kif4 and CENP-E. Phase 1/2. |
HeLa cells expressing iRFP were seeded onto 96-well plates and incubated with buffer or different concentrations of SB743921.During the next five days, the plate was scanned with an infrared imaging system (upper panel) to quantify the infrared signals (lower panel). |
|
| 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. |
|
| S7355 |
ARQ 621ARQ 621 is an allosteric, and selective Eg5 mitotic motor protein inhibitor. Phase 1. |
||
| S0279New |
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. |
||
| S6796New |
BTB-1BTB-1 is a novel, selective and reversible inhibitor of the mitotic motor protein Kif18A with IC50 of 1.69 μM. |
||
| S8439 |
MonastrolMonastrol 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. |
