产品描述:
I-BET762 (GSK525762A) is an inhibitor for BET (bromodomain and extra terminal domain) proteins, BRD2, BRD3 and BRD4. It binds to the tandem bromodomains of BET with a Kd of 50.5-61.3nM, displaces a tetra-acetylated H4 peptide prebound to tandem bromodomains of BET with IC50 of 32.5-42.5nM in FRET analysis. I-BET762 disrupts the formation of the chromatin complexes essential for expression of inflammatory genes.