tcsc2190 CPI-203

CPI-203 is a novel potent, selective and cell permeable inhibitor of BET bromodomain, with an IC₅₀ value of appr 37 nM (BRD4 α-screen assay).

IC50 & Target: IC50: 37 nM (BRD4)

In Vitro: CPI203 inhibits BRD4 in vitro and in cells, but 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].





In Vivo: BRD4 mediates CTD Ser2 phosphorylation in vivo^[1]. In REC-1 tumor-bearing mice, the combination of lenalidomide with CPI203 (2.5 mg/kg, i.p.) synergistically augments the antitumoral properties of each single agent via the abrogation of MYC and IRF4 expression and the induction of apoptosis^[2].