382194
HMTase Inhibitor VI, BRD4770
The HMTase Inhibitor VI, BRD4770 controls the biological activity of HMTase. This small molecule/inhibitor is primarily used for Cell Structure applications.
别名:
HMTase Inhibitor VI, BRD4770, EHMT2/G9a Inhibitor VI, Methyl-2-benzamido-1-(3-phenylpropyl)-1H-benzo[d]imidazole-5-carboxylate
质量水平
方案
≥98% (HPLC)
表单
powder
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
protect from light
颜色
white
溶解性
DMSO: 5 mg/mL
运输
ambient
储存温度
2-8°C
一般描述
A cell-permeable analog of the amino-benzimidazolo BIX-01338 (Cat. No. 539212 ) and the methylester prodrug of BRD9539 that acts as an SAM-competitive inhibitor against PRC2 and G9a (IC50 ≤6.3 µM) histone methyltransferase activities, displaying little effect toward 10 other HMTases, 9 HDACs, and 100 cellular kinases. Selectively reduces H3K9me2 and H3K9me3 (EC50 = 5 µM) histone methylation levels in pancreatic cancer cells (PANC-1) with much less or little effect toward H3K36me3, H3K4me3, H3K27me3, or H3K6me3 levels. Inhibits both anchorage-dependent and -independent PANC-1 proliferation via ATM activation and G2/M cell-cycle arrest, but not apoptosis induction (no caspase3/7 activation; 10 µM, 72 h).
生化/生理作用
Cell permeable: yes
Primary Target
G9a and PRC2 HMTases
G9a and PRC2 HMTases
Reversible: yes
包装
Packaged under inert gas
其他说明
Yuan, Y., et al. 2012. ACS Chem Biol.7, 1152.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Standard Handling (A)
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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