Mps1-IN-1 is a potent, selective, ATP-competitive Mps1 kinase inhibitor with IC50 and Kd of 367 nM and 27 nM.
Mps1-IN-1 also shows high affinity for ALK and LTK (Kd=21 and 39 nM), but shows little or no inhibition on other 352 member kinases.
Mps1-IN-1 induces checkpoint-mediated mitotic arrest in U2OS cells, disrupts recruitment of Mad2 to kinetochores, and reduces the phosphorylation status of Aurora B at threonine-232 (Thr232), suppresses the proliferative capacity of HCT116 cells.
