BRM014, BRM / BRG1 ATPase inhibitor

Product Details

Formal Name: 1-[3-(Difluoromethyl)isothiazol-5-yl]-3-[2-fluoro-5-(hydroxymethyl)pyridin-4-yl]urea

Molecular Formula: C₁₁H₉F₃N₄O₂S

Formula Weight: 318.3

CAS Number: 2270879-17-7

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (70 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

BRM / BRG1 ATPase inhibitor

Functions

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). 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.

Application Procedures

First dissolved in DMSO (70 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)