BRM012 (SMARCA2/SMARCA4 inhibitor 12) is a potent inhibitor of Brahma Homolog (BRM)/SMARCA2 and Brahma-related gene 1 (BRG1/SMARCA4) with IC50 of <5 nM for both.
BRM012 demonstrates cellular potency of KRT80 gene expression (reporter gene assay H1299 cells) and proliferation assays in BRG1-mutant SKMEL5 cells with AAC50 of 42 and 13 nM, respectively.
BRM012 is a small-molecule mSWI/SNF ATPase inhibitor, downregulates ACE2 and HNF1A expression and restrictes SARS-CoV-2 infection.
SWI/SNF-related, matrix-associated, actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2), also known as Brahma homologue (BRM), is a Snf2-family DNA-dependent ATPase. BRM and its close homologue Brahma-related gene 1 (BRG1), also known as SMARCA4, are mutually exclusive ATPases of the large ATP-dependent SWI/SNF chromatin-remodeling complexes involved in transcriptional regulation of gene expression.