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5.08320

Ezh2 Inhibitor III, SAH-EZH2

Name: Ezh2 Inhibitor III, SAH-EZH2
Brand: MM

别名:

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

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关于此项目

经验公式（希尔记法）:

C₁₅₅H₂₅₆N₄₈O₄₀ · 6CF₃CO₂H · XXH₂O

NACRES:

NA.77

UNSPSC Code:

12352200

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属性

assay

≥95% (HPLC)

Quality Segment

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

说明

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

Other Notes

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

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

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c