5.08320

Ezh2 Inhibitor III, SAH-EZH2

• Sinônimo(s): 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
• Fórmula empírica (Notação de Hill): C₁₅₅H₂₅₆N₄₈O₄₀ · 6CF₃CO₂H · XXH₂O
• Código UNSPSC: 12352200
• NACRES: NA.77

Propriedades

• Ensaio: ≥95% (HPLC)
• Nível de qualidade: 100
• forma: powder
• potência: 320 nM K_i
• fabricante/nome comercial: Calbiochem^®
• condição de armazenamento: OK to freeze; protect from light
• cor: white
• solubilidade: water: 100 mg/mL
• temperatura de armazenamento: −20°C

Descrição

Descrição geral

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.

Ações bioquímicas/fisiológicas

Cell permeable: yes

Primary Target
EED (embryonic ectoderm development) - EZH2

Embalagem

Packaged under inert gas

Advertência

Toxicity: Standard Handling (A)

Sequência

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

Outras notas

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

Informações legais

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

Informações de segurança

• Código de classe de armazenamento: 11 - Combustible Solids
• Classe de risco de água (WGK): WGK 3
• Ponto de fulgor (°F): Not applicable
• Ponto de fulgor (°C): Not applicable