5.08320

Ezh2 Inhibitor III, SAH-EZH2

• Synonym(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
• Empirical Formula (Hill Notation): C₁₅₅H₂₅₆N₄₈O₄₀ · 6CF₃CO₂H · XXH₂O
• UNSPSC Code: 12352200
• NACRES: NA.77

Properties

• assay: ≥95% (HPLC)
• Quality Level: 100
• form: powder
• potency: 320 nM K_i
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; protect from light
• color: white
• solubility: water: 100 mg/mL
• storage temp.: −20°C

Description

General description

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.

Biochem/physiol Actions

Cell permeable: yes

Primary Target
EED (embryonic ectoderm development) - EZH2

Packaging

Packaged under inert gas

Warning

Toxicity: Standard Handling (A)

Sequence

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

Other Notes

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

Legal Information

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

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk_germany: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable