SGC-SMARCA-BRDVIII

SGC-SMARCA-BRDVIII is a pan-inhibitor of family VIII bromodomain-containing proteins (BRDs), which are components of switch/sucrose nonfermentable (SWI/SNF) chromatin remodeling complexes. It selectively binds to polybromo-1D (PBRM1) bromodomain 5, BRM, also known as SMARCA2, and BRG1, also known as SMARCA4 (Kds = 13, 35, and 36 nM, respectively), over PBRM1 bromodomain 2, PBRM1 bromodomain 3, and PBRM1 bromodomain 4 (Kds = 3,655, 1,963, and >10,000 nM, respectively). SGC-SMARCA-BRDVIII (1 µM) decreases lipid accumulation induced by the PPARgamma agonist rosiglitazone (Cay-71740, Cay-11884, Cay-71742) in 3T3-L1 mouse fibroblasts differentiated into adipocytes by a combination of the phosphodiesterase (PDE) inhibitor IBMX (Cay-13347), the glucocorticoid dexamethasone (Cay-11015), and insulin. It decreases expression of the genes encoding PPARgamma, C/EBPalpha, and fatty acid binding protein 4 (FABP4), markers of adipocytes, in the same cells when used at a concentration of 0.5 µM. See the Structural Genomics Consortium (SGC) website for more information.Formal Name: 4-[3-amino-6-(2-hydroxyphenyl)-4-pyridazinyl]-1-piperazinecarboxylic acid, 1,1-dimethylethyl ester. CAS Number: 1997319-84-2. Molecular Formula: C19H25N5O3. Formula Weight: 371.4. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. lambdamax: 219, 265, 313 nm. SMILES: O=C(N1CCN(CC1)C2=C(N)N=NC(C3=CC=CC=C3O)=C2)OC(C)(C)C. InChi Code: InChI=1S/C19H25N5O3/c1-19(2,3)27-18(26)24-10-8-23(9-11-24)15-12-14(21-22-17(15)20)13-6-4-5-7-16(13)25/h4-7,12,25H,8-11H2,1-3H3,(H2,20,22). InChi Key: AQTNUGRRZDRZIA-UHFFFAOYSA-N.