Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC₅₀ and a K_d of 367 nM and 27 nM. IC50 & Target: IC50: 367 nM (Mps1)^[1]
Kd: 27 nM (Mps1)^[1] In Vitro: Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC₅₀ and a K_d of 367 nM and 27 nM. Mps1-IN-1 also has high affinity for ALK, and LTK, with K_ds of 21 and 39 nM, respectively, but shows little or no inhibition on other 352 member kinases. Mps1-IN-1 (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 (10 µM) shows no effect on centrosome duplication. In addition, Mps1-IN-1 (5-10 µM) suppresses the proliferative capacity of HCT116^[1].