Potent, SMARCA2/4 and PB1(5) BRDs-selective SWI/SNF bromodomain inhibitor that blocks adipogenesis with a >10-fold potency than PFI-3.
SGC-SMARCA-BRDVIII is a potent, SMARCA2/4 and PB1(bromo 5)-selective SWI/SNF bromodomain (BRD) inhibitor that effectively blocks adipocyte differentiation in 3T3-L1 murine fibroblast cultures (1 μM) by preventing the expression of key adipogenesis genes, including PPARγ, C/EBPα, and FABP4, with a >10-fold higher potency than PFI-3.
Journal of medicinal chemistry, 63(23), 14680-14699 (2020-11-21)
Accessibility of the human genome is modulated by the ATP-driven SWI/SNF chromatin remodeling multiprotein complexes BAF (BRG1/BRM-associated factor) and PBAF (polybromo-associated BAF factor), which involves reading of acetylated histone tails by the bromodomain-containing proteins SMARCA2 (BRM), SMARCA4 (BRG1), and polybromo-1.
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