Mps1-IN-2 is a potent, selective and ATP-competitive dual Mps1/Plk1 inhibitor, with an IC50 and a Kd of 145 nM and 12 nM for Mps1 and a Kd of 61 nM for Plk1.
IC50&Target
Mps1
12 nM (Kd)
GAK
140 nM (Kd)
PLK1
61 nM (Kd)
PLK3
1600 nM (Kd)
PLK4
3100 nM (Kd)
STK33
5000 nM (Kd)
体外研究
Mps1-IN-2 is a potent, selective and ATP-competitive Mps1 kinase inhibitor, with an IC50 and a Kd of 145 nM and 12 nM. Mps1-IN-2 also shows high affinity for PLK1 and GAK with Kds of 61 and 140 nM, respectively, but shows little or no inhibition on other 352 member kinases. Mps1-IN-2 can induces bypass of a checkpoint-mediated mitotic arrest in U2OS cells.
分子式
C26H36N6O3
分子量
480.60
CAS号
1228817-38-6
运输条件
Room temperature in continental US; may vary elsewhere.