产品说明
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 µM). 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 µM). 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-(4ʹ-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 |
产品性质
| 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 |
