Mps1-IN-1 dihydrochloride

Mps1-IN-1 dihydrochloride is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC ₅₀ and a K _d of 367 nM and 27 nM. Mps1-IN-1 dihydrochloride also has high affinity for ALK, and LTK, with K _d s of 21 and 39 nM, respectively, but shows little or no inhibition on other 352 member kinases. Mps1-IN-1 dihydrochloride (5, 10 μM) induces bypass of a checkpoint-mediated mitotic arrest in U2OS cells. Mps1-IN-1 disrupts recruitment of Mad2 to kinetochores, and reduces the phosphorylation status of Aurora B at threonine-232 (Thr232). Mps1-IN-1 dihydrochloride (10 µM) shows no effect on centrosome duplication. In addition, Mps1-IN-1 dihydrochloride (5-10 µM) suppresses the proliferative capacity of HCT116.