bs-83103C

DATASHEET

Formulation White solid

Storage: -20°C

Product Information:

SWI/SNF-related, matrix-associated, actin-dependent regulator of chromatin subfamily A member 2 (SMARCA2), also known as 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. BRM014 is an allosteric dual inhibitor of BRM and BRG1 (IC50<5 nM for both).1 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.2 For example, it reduced DNA accessibility to core regulatory factors (RUNX1, LM01 and MEIS1) at transcription factor PU.1 sites in AML cells.3 P583 cells formed markedly large spheroids when treated with BRM014.4 Cell permeable and active in vivo.

Description:

CAS Number: 2270879-17-7 Chemical Name: 1-[3-(Difluoromethyl)isothiazol-5-yl]-3-[2-fluoro-5-(hydroxymethyl)pyridine-4-yl]urea Molecular weight: 318.27 Formula: C11H9F3N4O2S Solubility: DMSO (70 mg/ml) Physical Properties: White solid Purity: >98% by HPLC NMR (Conforms)