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Ezh2 Inhibitor III, SAH-EZH2-Calbiochem
| 产品编号： | 4083525 |
| 规格： | 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. |
| 包装规格： | 2 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
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
基本信息
| Empirical Formula【经验(实验)分子式】 | C155H256N48O40 · 6C2HF3O2 · 14H2O |
| Molecular weight | 4368.34 |
| General description【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. |
| Biochem/physiol Actions【生化/生理作用】 | Cell permeable: yes Primary Target EED (embryonic ectoderm development) - EZH2 |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Sequence【序列】 | Ac-FSSNRXKILXRTQILNQEWKQRRIQPV (X=(S)-2-(4ʹ-pentenyl)Ala, stapled) |
| Other Notes【其他说明】 | Kim, W., et al. 2013. Nat. Chem. Biol.9, 643. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥95% (HPLC) |
| form【形式】 | powder |
| potency【效能】 | 320 nM Ki |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze protect from light |
| color【颜色】 | white |
| solubility【溶解性】 | water: 100 mg/mL |
| storage temp.【储存温度】 | −20℃ |
| packaging【包装】 | Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
