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FOCUS BIOMOLECULES BRM014, BRM / BRG1 ATPase inhibitor, CAS# 2270879-17-7, >98% by HPLC_NMR (Conforms)
Supplier: FOCUS BIOMOLECULES 1052441MG
Biochemical Reagents, BRM014, BRM / BRG1 ATPase inhibitor, CAS# 2270879-17-7, >98% by HPLC_NMR (Conforms), SWI/SNF-related, matrix-associated, actin-dependent regulator of chromatin subfamily A member 2 [SMARCA2, or Brahma homologue (BRM)], together with its close homologue Brahma-related gene 1 (BRG1), or SMARCA4, are ATPases of the large ATP-dependent SWI/SNF chromatin-remodeling complexes involved in transcriptional regulation of gene expression. Allosteric dual inhibitor of BRM & BRG1 (IC50<5 nM for both). It downregulated BRM-dependent gene expression and displayed antiproliferative activity in a BRG1-mutant-lung-tumor xenograft model after oral administration. Inhibition of BRG1/BRM ATPase by BRM014 inhibits chromatin openness. For example, it reduced DNA accessibility to core regulatory factors (RUNX1, LM01 and MEIS1) at transcription factor PU.1 sites in AML cells. P583 cells formed markedly large spheroids when treated with BRM014. Cell permeable and active in vivo.
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