CPI203 是一种选择性的，细胞通透的BET 溴结构域抑制剂，抑制BRD4，IC50值约为 37 nM。

CPI-203 is an effective BET bromodomain inhibitor (IC50: 37 nM for BRD4).

CPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro. [1] 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. Furthermore, lenalidomide and CPI203, by targeting IRF4 and MYC, efficiently activates the cell death program in MCL cells resistant to bortezomib. [2]

BRD4 α-screen assay: The BRD4 α-screen assay is a proximity-based assay using a tetraacteylated H4 peptide and the isolated bromodomain 1 of human BRD4. IC50 values are calculated using a 10-point serial dilution of BET inhibitor.

1446144-04-2

C19H18ClN5OS

399.9

CPI 203;CPI203

DMSO:72 mg/mL(180 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years