您好,欢迎来到半岛电竞官方网址 ! [ 登录] [ 免费注册]
半岛电竞官方网址
位置: 首页> 品牌> Sigma-Aldrich> Ezh2 Inhibitor II, EI1-CAS 1418308-27-6-Calbiochem

Ezh2 Inhibitor II, EI1-CAS 1418308-27-6-Calbiochem

品牌
Sigma-Aldrich
CAS
1418308-27-6
货号
5.00561
包装型号
规格纯度
价格
2579.1 *本价格含增值税费
促销
服务
  • 原厂保证
  • 包邮
  • 增值税票
数量
- +
半岛bd体育手机客户端 名称:
1418308-27-6
Ezh2 Inhibitor II, EI1-CAS 1418308-27-6-Calbiochem
Enhancer of Zested Homolog 2 Inhibitor II, HMTase Inhibitor XI, 6-Cyano-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-1-(pentan-3-yl)-1H-indole-4-carboxamide
半岛bd体育手机客户端 介绍:

半岛bd体育手机客户端 说明

一般描述

A cell-permeable indolocarboxamide compound that acts as a potent and selective inhibitor against Ezh2/PRC2 (Polycomb repressive complex 2; Ezh2/SUZ12/EED/AEBP2/RbAP48) HMTase activity (IC50/substrate = 15 nM/H3K27me021-44and 13 nM/H3K27me221-44, respectively, against human wt or Y641F Ezh2-containing PRC2; [SAM] = 1 ?M) in a cofactor SAM-competitive manner, while inhibiting Ezh1/PRC2 only at much higher concentrations (IC50= 1.34 ?M) and exhibiting no potency toward CARM 1, Dot1L, G9a, MLL, NSD3, Set7/9, SETD2, SETD8, SmyD2, or Suv39H2 (IC50>100 ?M). Shown to selectively suppress cellular H3K27 dimethylation and trimethylation (1 to 10 ?M in 1 to 5 days) in DLBCL (diffuse large B cell lymphoma) cultures, but not those of H3K4, H3K9, H3K36, or H3K79. EI1 is shown to exhibit antiproliferation activity against DLBCL cell lines with wt- (by 90% in G401 with 3.3 ?M EI1; by 78% in Toledo with 10 ?M EI1; 14 d incubation) or mutant- Ezh2 (by >96% in WSU-DLCL2/Y641F, SU-DHL6/Y641N, Karpas422/Y641N, and DB/Y641N cultures with 3.3 ?M EI1; by >96% in SU-DHL4 cultures with10 ?M EI1; 14 d incubation), while being less effective against MEF (by 40% in 11 days at 3.3 ?M) and ineffective toward wt Ezh2-expressing GA10 and OCI-LY19.
A cell-permeable indolocarboxamide compound that acts as a potent and selective inhibitor against Ezh2/PRC2 (Polycomb repressive complex 2; Ezh2/SUZ12/EED/AEBP2/RbAP48) HMTase activity (IC50/substrate = 15 nM/H3K27me021-44and 13 nM/H3K27me221-44, respectively, against human wt or Y641F Ezh2-containing PRC2; [SAM] = 1 ?M) in a cofactor SAM-competitive manner, while inhibiting Ezh1/PRC2 only at much higher concentrations (IC50= 1.34 ?M) and exhibiting no potency toward CARM 1, Dot1L, G9a, MLL, NSD3, Set7/9, SETD2, SETD8, SmyD2, or Suv39H2 (IC50>100 ?M). Shown to suppress cellular H3K27 dimethylation and trimethylation (1 to 10 ?M) in DLBCL cultures and exhibit antiproliferation activity against DLBCL cell lines with wt or mutant Ezh2 (3.3 ?M to 10 ?M).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

生化/生理作用

Cell permeable: yes
Primary Target
Ezh2/PRC2
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

其他说明

Qi, W., et al. 2012.Proc. Natl. Acad. Sci. USA.109,21360.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式 C23H26N4O2
分子量 390.48

半岛bd体育手机客户端 性质

质量水平 100
测定 ≥98% (HPLC)
形式 solid
manufacturer/tradename Calbiochem?
储存条件 OK to freeze
protect from light
颜色 white
溶解性 DMSO: 10 mg/mL
储存温度 2-8℃

安全信息

储存分类代码 11 - Combustible Solids
WGK WGK 2

Sigma-Aldrich

推荐半岛bd体育手机客户端
Baidu
map