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K858 (Racemic) is an ATP-uncompetitive inhibitor of kinesin Eg5 with an IC50 of 1.3 μM. Eg5 is a key protein involved in the formation of bipolar spindles. K858 induces mitotic arrest, caspase-3 activation and cell growth inhibition in HCT116 cells. K858 (5 μM) induces mitotic cell death in cancer cells but not in normal cells. K858 (1, 10, 100 μM) inhibits the MCF7, BT474 and SKBR3 cell lines, and only at 10 and 100 μM suppresses MDA-MB231 cell line after treatment for 24 h. K858 incereases Bax/Bcl2 RNA ratio and survivin in the four cell lines.
| Molecular Weight | 277.34 |
| Formula | C13H15N3O2S |
| CAS Number | 72926-24-0 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Kinesin Products |
|---|
| Ispinesib
Ispinesib (SB 715992) is the first potent, highly specific small-molecule inhibitor of kinesin spindle protein (KSP) with an IC50 of 4.1 nM. |
| SB-743921
SB-743921 is a highly potent and active KSP inhibitor with a Ki of 0.1 nM for KSP (Eg5). |
| AZ3146
AZ3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor with IC50 of 35 nM. |
| GSK923295
GSK923295 is an allosteric inhibitor of CENP-E with Ki value of 3.2 nM. |
| MPI-0479605
MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase Mps1 with IC50 of 1.8 nM, >40-fold selectivity over other kinases. |
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Products are for research use only. Not for human use. We do not sell to patients.
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