1883548-93-3
1883548-93-3 結(jié)構(gòu)式
常見(jiàn)問(wèn)題列表
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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 (IC 50 ) |
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.