5.08320

Ezh2 Inhibitor III, SAH-EZH2

• 동의어(들): 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
• 실험식(Hill 표기법): C₁₅₅H₂₅₆N₄₈O₄₀ · 6CF₃CO₂H · XXH₂O
• UNSPSC 코드: 12352200
• NACRES: NA.77

속성

• 분석: ≥95% (HPLC)
• Quality Level: 100
• 형태: powder
• 효능: 320 nM K_i
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: white
• solubility: water: 100 mg/mL
• 저장 온도: −20°C

설명

일반 설명

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.

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
EED (embryonic ectoderm development) - EZH2

포장

Packaged under inert gas

경고

Toxicity: Standard Handling (A)

서열

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

기타 정보

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

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable