CPI-203
M3526
Brand
No Brand
Description
CPI-203 is a potent, selective and cell permeable inhibitor of the bromodomain and extra terminal (BET) family protein BRD4 with an IC50 of ~37 nM. CPI-203 inhibits BRD4 in vitro and in cells, but it does not affect BRD4 kinase activity in vitro. CPI203 exerts a cytostatic effect in all the 9 MCL cell lines analyzed with GI50 ranging from 0.06 to 0.71 μM), with low cytotoxicity in normal PBMCs from healthy donors. CPI-203 arrests the growth of leukemic T cells in vitro (EC50 = 91 nM) and rapidly suppresses leukemia burden in mice. In contrast, in vivo, specific Ser2 phosphorylation by either endogenous BRD4 or exogenous BRD4 FEE-AAA was markedly decreased by treatment with the inhibitor.
Application
Reactivity
