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BRM012

Chemical Structure : BRM012

CAS No.: 2270879-43-9

BRM012 (BRM-012, SMARCA2/SMARCA4 inhibitor 12)

Catalog No.: PC-20119Not For Human Use, Lab Use Only.

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.

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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 334.73
    Formula C11H9ClF2N4O2S
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20°C 12 Months; 4°C 6 Months
    In Solvent
    -80°C 6 Months; -20°C 6 Months
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    1-(2-chloro-5-(hydroxymethyl)pyridin-4-yl)-3-(3-(difluoromethyl)isothiazol-5-yl)urea

    References

    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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