Molecular Weight(MW): 399.90
CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.
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Choose Selective Epigenetic Reader Domain Inhibitors
|Description||CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.|
CPI203 inhibits BRD4 in vitro and in cells, while 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. Furthermore, lenalidomide and CPI203, by targeting IRF4 and MYC, efficiently activates the cell death program in MCL cells resistant to bortezomib. 
|In vivo||BRD4 mediates CTD Ser2 phosphorylation in vivo.  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. |
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.
|In vitro||DMSO||79 mg/mL warmed (197.54 mM)|
|Ethanol||5 mg/mL (12.5 mM)|
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