Empesertib (BAY-1161909, BAY1161909) is a potent, selective Monopolar spindle 1 (Mps1/TTK) inhibitor with IC50 of 0.34 nM.
BAY1161909 inhibits only JNK2 and JNK3 more than 50% at 1 uM in Millipore panel (230 kinases).
BAY1161909 abrogates nocodazole-induced metaphase arrest in HeLa cells with IC50 of 56 nM, inhibits the proliferation of a panel tumor cell lines covering various cancer with mean IC50 of 160 nM.
BAY1161909 enhances the efficacy of antimitotic cancer drugs and shows potentially overcome resistance in vivo.
