iBET-BD2

iBET-BD2 is an inhibitor of the bromodomain and extra-terminal domain (BET) family protein bromodomain 2 (BD2). It inhibits BD2 in bromodomain-containing protein 2 (BRD2), BRD3, BRD4, and BRDT (IC50s = 264, 98, 49, and 214 nM, respectively) and is selective for BD2 over BD1 (IC50s = 10.96, 36.31, 70.55, and >50.11 µM for BRD2, BRD3, BRD4, and BDT, respectively) in a time-resolved FRET (TR-FRET) assay. iBET-BD2 (1 µM) inhibits IFN-gamma-induced protein expression of MHC class I in K562 cells. It reduces the production of anti-KLH IgM antibodies in mice immunized with keyhole limpet hemocyanin (KLH) when administered at a dose of 40 mg/kg.Formal Name: 4-(acetylamino)-3-fluoro-N-(trans-4-hydroxycyclohexyl)-5-[(1S)-1-phenylethoxy]-benzamide. CAS Number: 2474876-09-8. Synonyms: GSK046. Molecular Formula: C23H27FN2O4. Formula Weight: 414.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMSO: soluble. lambdamax: 253 nm. SMILES: O[C@H]1CC[C@H](NC(C2=CC(F)=C(NC(C)=O)C(O[C@@H](C)C3=CC=CC=C3)=C2)=O)CC1. InChi Code: InChI=1S/C23H27FN2O4/c1-14(16-6-4-3-5-7-16)30-21-13-17(12-20(24)22(21)25-15(2)27)23(29)26-18-8-10-19(28)11-9-18/h3-7,12-14,18-19,28H,8-11H2,1-2H3,(H,25,27)(H,26,29)/t14-,18-,19-/m0/s1. InChi Key: FRBRZGLUFOZRGD-JVPBZIDWSA-N.