GSK6853

GSK6853 is a chemical probe for the bromodomain of BRPF1 that displays a TR-FRET pIC50 value of 8.1 and a BROMOscan pKd value of 9.5. It exhibits >1,600-fold selectivity for BRPF1 over all other bromodomains in a BROMOscan assay and shows cellular target engagement with a pIC50 value of 7.7 in a NanoBRET assay evaluating the interaction of the NanoLuc-BRPF1 bromodomain with histone H3.3-HaloTag in HEK293 cells. See the Structural Genomics Consortium (SGC) website for more information.Formal Name: N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxy-benzamide. CAS Number: 1910124-24-1. Molecular Formula: C22H27N5O3. Formula Weight: 409.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/mL, DMSO: 25 mg/mL, Ethanol: 30 mg/mL, Ethanol:PBS(pH 7.2) (1:1): 0.5 mg/mL. lambdamax: 239, 318 nm. SMILES: C[C@H](CNCC1)N1C2=C(NC(C3=CC=CC=C3OC)=O)C=C4C(N(C)C(N4C)=O)=C2. InChi Code: InChI=1S/C22H27N5O3/c1-14-13-23-9-10-27(14)17-12-19-18(25(2)22(29)26(19)3)11-16(17)24-21(28)15-7-5-6-8-20(15)30-4/h5-8,11-12,14,23H,9-10,13H2,1-4H3,(H,24,28)/t14-/m1/s1. InChi Key: FQWDVNSBYDXPIO-CQSZACIVSA-N.