pan-bd2

BET-IN-17, also known as compound 16, serves as a pan-inhibitor for BET, exhibiting inhibitory potencies (pIC50) of 7.8 for BET BD1 and 7.6 for BET BD2 [1].

I-BET282E is a pan-inhibitor of eight BET bromodomains and shows selectivity for other representative bromodomain-containing proteins. It can act on eight BRD2 (BD1 BD2), BRD2 (BD1 BD), BRD3 (BD1 BD), and BRD4 (BD1 BD), with their pIC50 values ranging from 6.4 to 7.7.

GSK620 is a pan-BD2 inhibitor, which shows an anti-inflammatory phenotype in human whole blood with excellent broad selectivity, developability, and in vivo oral pharmacokinetics.GSK620 is highly selective for the BET-BD2 family of proteins, with >200-fol

XY221 (Compound 16o) selectively inhibits BRD4 BD2 with an IC50 of 5.8 nM. It demonstrates high selectivity for pan-BD2 and BRD4 BD2 domains, being 667 times more selective than for BRD4 BD1, and 9-32 times more selective than for BRD2 3 T BD2. XY221 can induce apoptosis in MV4-11 cells and exhibits anti-cancer activity.

I-BET567, a potent pan-BET inhibitor with oral activity, demonstrates pIC50 values of 6.9 and 7.2 for BRD4 BD1 and BD2, respectively. This compound has exhibited efficacy in mouse models of oncology and inflammation [1].