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Ezh2 Inhibitor III, GSK126

品牌
Sigma-Aldrich
货号
5.00580
规格纯度
A cell-permeable structural analog of E1 that acts as an equipotent, SAM-competitive inhibitor of Ezh2/PRC2 inhibitor (Ki= 0.5 to 3 nM against wt &mutant Ezh2-containing PRC2).
价格
3557.45 *本价格含增值税费
促销
服务
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数量
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半岛bd体育手机客户端 名称:
Ezh2 Inhibitor III, GSK126
Enhancer of Zested Homolog 2 Inhibitor III, ( S)-1-( sec-Butyl)-N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-3-methyl-6-(6-(piperazin-1-yl)pyridin-3-yl)-1 H-indole-4-carboxamide, HMTase Inhibitor XIV
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 EI1 (Cat. No. 500561) structural analog that acts as an equally potent, SAM-competitive, Ezh2/PRC2 inhibitor (Ki= 0.5 to 3 nM against wt, A677G, Y641F, Y641H, Y641N, Y641S, Y641C Ezh2-containing PRC2; [SAM] = 7.5 ?M) with similar selectivity over Ezh1/PRC2 (Ki= 89 nM) and other HTMases as EI1. Among panels of 14 HDACs, 11 GPCRs, and 300 kinases, only serotonin 3 receptors, JMJD2d, and CaMK1a are significantly inhibited at much higher concentrations (IC50= 4, 7.9, and ≥10 ?M, respectively). In addition to DLBCL (diffuse large B cell lymphoma; IC50ranges from 28 nM to 5.5 ?M; 6 d treatment), GSK126 is also shown to inhibit the proliferation of other B-NHL (non-Hodgkin′s lymphoma) and Hodgkin′s lymphoma cell lines, being least active against MC116, HD-MY-Z, WSU-FSCCL, Toledo, NU-DUL-1, and WILL-2 (IC50>10 ?M; 6 d treatment). When administered at a daily i.p. dose of 50 mg/kg GSK126 is reported to completely suppress Pfeiffer (A677G) and Karpas-422 (Y641N) tumor expansion in micein vivo, while complete tumor eradication can be achieved with higher dosing regimens (150 mg/kg/day or two 300 mg/kg dosages per week).
A cell-permeable EI1 (Cat. No. 500561) structural analog that acts as an equally potent, SAM-competitive, Ezh2/PRC2 inhibitor (Ki= 0.5 to 3 nM against wt & mutant Ezh2-containing PRC2; [SAM] = 7.5 ?M) with similar selectivity over Ezh1/PRC2 (Ki= 89 nM) and other HTMases as EI1. Among panels of 14 HDACs, 11 GPCRs, and 300 kinases, only serotonin 3 receptor, JMJD2d, and CaMK1a are significantly inhibited at much higher concentrations (IC50≥4 ?M). Shown to inhibit the proliferation of DLBCL (IC5028 nM to 5.5 ?M; 6 d treatment)in vitroand completely suppress Pfeiffer (A677G) and Karpas-422 (Y641N) tumor expansion in micein vivo(50 mg/kg/d i.p.).

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.

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.
Use only fresh DMSO for reconstitution.

其他说明

McCabe, M.T., et al. 2012.Nature.492,108.

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 C31H38N6O2
分子量 526.67

半岛bd体育手机客户端 性质

质量水平 100
测定 ≥98% (HPLC)
形式 semisolid
manufacturer/tradename Calbiochem?
储存条件 OK to freeze
protect from light
颜色 brown
溶解性 DMSO: 10 mg/mL
储存温度 ?20℃

安全信息

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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