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Chemical Structure : Dual BRM and BRG1 inhibitor 12
Catalog No.: PC-20119Not For Human Use, Lab Use Only.
Dual BRM and BRG1 inhibitor 12 (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.
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Dual BRM and BRG1 inhibitor 12 (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.
Dual BRM and BRG1 inhibitor 12 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.
Dual BRM and BRG1 inhibitor 12 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.
| M.Wt | 334.73 | |
| Formula | C11H9ClF2N4O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Wei J, et al. Nat Genet. 2023 Mar 9. doi: 10.1038/s41588-023-01307-z.
2. Julien P N Papillon, et al. J Med Chem. 2018 Nov 21;61(22):10155-10172.
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