Mps1-IN-1 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 367 nM and 27 nM.
IC50&Target
Mps1
367 nM (IC50)
Mps1
27 nM (Kd)
ALK
21 nM (Kd)
LTK
29 nM (Kd)
PYK2
280 nM (Kd)
FAK
440 nM (Kd)
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)
体外研究
Mps1-IN-1 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 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 (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.
分子式
C28H33N5O4S
分子量
535.66
CAS号
1125593-20-5
运输条件
Room temperature in continental US; may vary elsewhere.