GSK 525762A is an inhibitor for BET (bromodomain and extra terminal domain) proteins, BRD2, BRD3 and BRD4, binds to the tandem bromodomains of BET with Kd of 50.5-61.3 nM, displaces
a tetra-acetylated H4 peptide prebound to tandem bromodomains of BET with IC50 of 32.5-42.5 nM in FRET analysis. GSK 525762A occupies the acetyl-lysine binding pocket of BET proteins and inhibits
binding of BET proteins to acetylated histones, thus disrupts the formation of the chromatin complexes essential for expression of inflammatory genes.