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Ezh2 Inhibitor III, SAH-EZH2-Calbiochem

品牌
Sigma-Aldrich
货号
5.08320
规格纯度
A helical 27-mer peptide with E54Q modification that directly binds to EDD (Kd = 320 nM) and disrupts protein-protein interaction of EED with EZH2 and EZH1.
价格
4209.84 *本价格含增值税费
促销
服务
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  • 包邮
  • 增值税票
数量
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半岛bd体育手机客户端 名称:
Ezh2 Inhibitor III, SAH-EZH2-Calbiochem
H3K27 Methylation Inhibitor, SAH-EZH2, EED-EZH2 Protein-Protein Interaction Inhibitor, SAH-EZH2, Enhancer of Zested Homolog 2 Inhibitor III, 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 stabilized a-helical 27-mer peptide (FSSNRXKILXRTQILNQEWKQRRIQPV) with E54Q modification that exhibits robust cellular uptake and nuclear localization and directly binds to embryonic ectoderm development (EED; Kd= 320 nM) and disrupts protein-protein interaction of EED with EZH2 ( Enhancer of zeste homolog 2 ) and EZH1. Selectively inhibits methyltransferase activity of the Polycomb repressive complex 2 (PRC2) and reduces H3K27 methylation in a dose-dependent manner (~1 to 10 ?M). Induces growth arrest at the Go/G1 phase (after 6 days of treatment) and monocyte-macrophage differentiation in MLL-AF9 leukemia cells without inducing any apoptosis. Growth arrest is suggested to be associated with an increase in p19ARF levels. Shown to block the proliferation of C1498 and M1 myeloid leukemia cells without affecting non-tumorigenic HPC5 cells.
A stabilized a-helical 27-mer peptide (FSSNRXKILXRTQILNQEWKQRRIQPV) with E54Q modification that exhibits robust cellular uptake and nuclear localization and directly binds to embryonic ectoderm development (EED; Kd= 320 nM) and disrupts protein-protein interaction of EED with EZH2 ( Enhancer of zeste homolog 2 ) and EZH1. Selectively inhibits methyltransferase activity of the Polycomb repressive complex 2 (PRC2) and reduces H3K27 methylation in a dose-dependent manner (~1 to 10 ?M). Induces growth arrest at the Go/G1 phase (after 6 days of treatment) and monocyte-macrophage differentiation in MLL-AF9 leukemia cells without inducing any apoptosis. Growth arrest is suggested to be associated with an increase in p19ARF levels. Shown to block the proliferation of C1498 and M1 myeloid leukemia cells without affecting non-tumorigenic HPC5 cells.

Please note that the molecular weight for this compound is batch-specific due to variable water content.

生化/生理作用

Cell permeable: yes
Primary Target
EED (embryonic ectoderm development) - EZH2

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

序列

Ac-FSSNRXKILXRTQILNQEWKQRRIQPV (X=(S)-2-(4?-pentenyl)Ala, stapled)

其他说明

Kim, W., et al. 2013.Nat. Chem. Biol.9,643.

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 C155H256N48O40· 6C2HF3O2· 14H2O
分子量 4368.34

半岛bd体育手机客户端 性质

质量水平 100
测定 ≥95% (HPLC)
形式 powder
效能 320 nM Ki
manufacturer/tradename Calbiochem?
储存条件 OK to freeze
protect from light
颜色 white
溶解性 water: 100 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

Sigma-Aldrich

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