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The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, affect inflammatory gene expression by controlling the assembly of histone acetylation-dependent chromatin complexes. I-BET762 is a synthetic compound which interacts with BET proteins with high-affinity (Kd = 32.5-42.5 nM). It blocks binding of BET proteins with acetylated histones, disrupting the formation of chromatin complexes involved in the expression of specific inflammatory genes in activated macrophages. Through these actions, I-BET762 provides protection against bacteria-induced sepsis and lipopolysaccharide-triggered endotoxic shock.Formal Name: (S)-2-(6-(4-chlorophenyl)-8-methoxy-4H-benzo[f][1,2,4]triazolo[4,3-a][1,4]diazepin-4-yl)-N-ethylacetamide. CAS Number: 1260907-17-2. Synonyms: GSK525762A. Molecular Formula: C22H22ClN5O2. Formula Weight: 423.9. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 20 mg/ml, Ethanol: 30 mg/ml, Ethanol:PBS (pH 7.2) (1:1): 0.5 mg/ml. SMILES: COC1=CC(C(C2=CC=C(Cl)C=C2)=N[C@H]3CC(N(CC)[H])=O)=C(N4C3=NN=C4C)C=C1. InChi Code: InChI=1S/C22H22ClN5O2/c1-4-24-20(29)12-18-22-27-26-13(2)28(22)19-10-9-16(30-3)11-17(19)21(25-18)14-5-7-15(23)8-6-14/h5-11,18H,4,12H2,1-3H3,(H,24,29)/t18-/m0/s1. InChi Key: AAAQFGUYHFJNHI-SFHVURJKSA-N.
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