5.08320

Ezh2 Inhibitor III, SAH-EZH2

• Synonim(y): 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
• Wzór empiryczny (zapis Hilla): C₁₅₅H₂₅₆N₄₈O₄₀ · 6CF₃CO₂H · XXH₂O
• Kod UNSPSC: 12352200
• NACRES: NA.77

Właściwości

• Próba: ≥95% (HPLC)
• Poziom jakości: 100
• Postać: powder
• siła działania: 320 nM K_i
• producent / nazwa handlowa: Calbiochem^®
• warunki przechowywania: OK to freeze; protect from light
• kolor: white
• rozpuszczalność: water: 100 mg/mL
• temp. przechowywania: −20°C

Opis

Opis ogólny

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.

Działania biochem./fizjol.

Cell permeable: yes

Primary Target
EED (embryonic ectoderm development) - EZH2

Opakowanie

Packaged under inert gas

Ostrzeżenie

Toxicity: Standard Handling (A)

Sekwencja

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

Inne uwagi

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

Informacje prawne

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

Informacja o środkach bezpieczeństwa

• Kod klasy składowania: 11 - Combustible Solids
• Klasa zagrożenia wodnego (WGK): WGK 3
• Temperatura zapłonu (°F): Not applicable
• Temperatura zapłonu (°C): Not applicable