5.08320

Ezh2 Inhibitor III, SAH-EZH2

• 別名: Ezh2 Inhibitor III, SAH-EZH2, H3K27 Methylation Inhibitor, SAH-EZH2, EED-EZH2 Protein-Protein Interaction Inhibitor, SAH-EZH2, Enhancer of Zested Homolog 2 Inhibitor III, HMTase Inhibitor XIV
• 実験式（ヒル表記法）: C₁₅₅H₂₅₆N₄₈O₄₀ · 6CF₃CO₂H · XXH₂O
• UNSPSCコード: 12352200
• NACRES: NA.77

特性

• アッセイ: ≥95% (HPLC)
• 品質水準: 100
• 形状: powder
• 有効性: 320 nM K_i
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: white
• 溶解性: water: 100 mg/mL
• 保管温度: −20°C

詳細

詳細

Ezh2 Inhibitor III, SAH-EZH2 is a stabilizeda-helical 27-mer peptide (FSSNRXKILXRTQILNQEWKQRRIQPV )with E54Q modification. It shows strong cellular uptake and nuclearlocalization and directly forms a complex during embryonic ectodermdevelopment. It blocks the protein-protein interaction of embryonic ectoderm development(EED) with enhancer of zeste homolog (EZH) 1 and 2. Selectively inhibits methyltransferase activity of the Polycombrepressive complex 2 (PRC2) and reduces H3K27 methylation in a dose-dependentmanner (~1 to 10 µM). This inhibitor induces growth arrest after six days oftreatment at the G0/G1 phase and monocyte-macrophage differentiation in MLL-AF9leukemia cells without inducing any apoptosis. The growth arrest is suggestedto be associated with an increase in p19ARF levels. It blocks the proliferationof M1 myeloid leukemia cells and C1498 without having any effect onthe non-tumorigenic HPC5 cells.

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
EED (embryonic ectoderm development) - EZH2

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

シーケンス

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

その他情報

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

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable