I-BET-762 CAS:1260907-17-2 is a benzodiazepine, cell-permeable BET protein inhibitor that binds to the tandem bromodomains (bromodomain and extra terminal domain) of BET. I-BET-762 binds to BRD2 (1-473), BRD3 (1-434) and BRD4 (1-477) with high affinity (ITC Kd = 61.3, 50.5 and 55.2 nM, respectively) and competes effectively against BRD2/3 /4 binds the tetraacetylated H4 peptide (IC50 = 32.5, 42, 4 and 36.1 nM, respectively) and has little affinity for the other 5 bromodomain-containing proteins (ATAD2, BAZ2B, CREBBP, PCAF, SP140) . I-BET-762 has been reported to downregulate the expression of LPS-induced genes, resulting in decreased LPS-induced expression of cytokines and chemokines.
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