I-BET 762

I-BET 762

I-BET-762 is cell-permeable benzodiazepine compound that binds the tandem bromodomains of BET (bromodomain and extra terminal domain). I-BET-762 binds to BRD2 (1-473), BRD3 (1-434), and BRD4 (1-477) with high affinity (Kd = 61.3, 50.5, and 55.2 nM, respectively, by ITC) and effectively competes against tetra-acetylated H4 peptide for BRD2/3/4 binding (IC50 = 32.5, 42,4, and 36.1 nM, respectively), while exhibiting little affinity toward 5 other bromodomain-containing proteins (ATAD2, BAZ2B, CREBBP, PCAF, SP140). I-BET-762 is reported to downregulate the expression of the genes which are induced by LPS, thus causing the decreased expression of LPS-inducible cytokines and chemokines.