MK-0731 is a potent, selective kinesin spindle protein (KSP) inhibitor with IC50 of 2.2 nM, cell EC50 of 5.3 nM.
MK-0731 dispalys >20,000-fold selectivity for KSP over a panel of eight related kinesins (CENP-E, MKLP-1, Kif3A, Kif1B, uKHC, nKHC, KIF14, and MCAK).
MK-0731 induces a mitotic block with an IC50 of 19 nM in cells that are refractory to paclitaxel due to P-gp overexpression.
MK-0731 induces dose-dependent mitotic arrest in tumors and inhibits tumor growth in mouse xenograft.
