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.¹ It selectively binds to polybromo-1D (PBRM1) bromodomain 5, BRM, also known as SMARCA2, and BRG1, also known as SMARCA4 (K_ds = 13, 35, and 36 nM, respectively), over PBRM1 bromodomain 2, PBRM1 bromodomain 3, and PBRM1 bromodomain 4 (K_ds = 3,655, 1,963, and >10,000 nM, respectively). SGC-SMARCA-BRDVIII (1 µM) decreases lipid accumulation induced by the PPARγ agonist rosiglitazone (Item Nos. 71740 | 11884 | 71742) in 3T3-L1 mouse fibroblasts differentiated into adipocytes by a combination of the phosphodiesterase (PDE) inhibitor IBMX (Item No. 13347), the glucocorticoid dexamethasone (Item No. 11015), and insulin. It decreases expression of the genes encoding PPARγ, C/EBPα, 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.

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1. Wanior, M., Preuss, F., Ni, X., et al. Pan-SMARCA/PB1 bromodomain inhibitors and their role in regulating adipogenesis. J. Med. Chem. 63(23), 14680-14699 (2020).