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