Ispinesib (SB-715992) is a potent, selective, cell-permeable, allosteric inhibitor of Eg5 (mitotic kinesin KSP) with Ki of 2.3 nM.
Ispinesib (SB-715992) displays >10,000-fold selectivity for Eg5 over a range of other mitotic kinesins.
Ispinesib (SB-715992) 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.
Ispinesib (SB-715992) demonstrates tumor regression of breast cancer cell xenografts in mice at 10 mg/kg.
