GSK-923295 (GSK923295) is the first potent, allosteric inhibitor of CENP-E kinesin motor ATPase activity with Ki of 3.2 nM.
GSK-923295 shows excellent selectivity against a panel of mitotic human kinesins.
GSK-923295 exhibits inhibition of cell proliferation in a broad panel of human cancer cell lines and induces mitotic arrest leading to apoptosis and cell death (SKOV-3 IC50=22 nM; Colo205 IC50=22 nM).
GSK-923295 induces tumor regressions in vivo.
