Mps1-IN-1 dihydrochloride

Mps1-IN-1 dihydrochloride is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM[1].

Research Areas >> Cancer

Signaling Pathways >> Cytoskeleton >> Mps1

Signaling Pathways >> Cell Cycle/DNA Damage >> Mps1

Mps1:27 nM (Kd)

ALK:21 nM (Kd)

LTK:29 nM (Kd)

PYK2:280 nM (Kd)

FAK:440 nM (IC30)

IGF1R:750 nM (Kd)

INSR:470 nM (Kd)

CLK1:1900 nM (Kd)

ERK2:2900 nM (Kd)

INSRR:1200 nM (Kd)

TNK1:2600 nM (Kd)

TNK2:3100 nM (Kd)

GAK:1100 nM (Kd)

Mps1:367 nM (IC50)

Mps1-IN-1 dihydrochloride is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM. Mps1-IN-1 dihydrochloride also has high affinity for ALK, and LTK, with Kds 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[1].

[1]. Kwiatkowski N, et al. Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. Nat Chem Biol. 2010 May;6(5):359-68.