K858

K858 is an inhibitor of kinesin spindle protein Eg5 (IC₅₀ = 1.3 µM for Eg5 ATPase activity).¹ It inhibits growth (GI₅₀ = 0.98 µM), induces mitotic arrest (EC₅₀ = 1.6 µM), and activates caspase-3 (EC₅₀ = 1.6 µM) in HCT116 cells. It selectively induces mitotic cell death in HCT116 cells over non-cancerous ARPE-19 retinal pigment epithelial cells. K858-treated HCT116 cells that escape mitotic cell death undergo polyploidization and senescence. K858 reduces tumor growth in an A2780 ovarian cancer mouse xenograft model when administered at a dose of 150 mg/kg and increases the number of mitotic cells with monopolar spindles in tumor tissue.

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1. Nakai, R., Iida, S., Takahashi, T., et al. K858, a novel inhibitor of mitotic kinesin Eg5 and antitumor agent, induces cell death in cancer cells. Cancer Res. 69(9), 3901-3909 (2009).