化合物CPI203 T6026

Product Introduction
Bioactivity


英文名: CPI-203

描述: CPI-203 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。

激酶实验: 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.

体外活性: 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]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 72 mg/mL(180 mM)


关键字: CPI-203 | Epigenetic Reader Domain | Inhibitor | Apoptosis | inhibit

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