5.08320
Ezh2 Inhibitor III, SAH-EZH2
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
assay
≥95% (HPLC)
form
powder
potency
320 nM Ki
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
white
solubility
water: 100 mg/mL
storage temp.
−20°C
Quality Level
Biochem/physiol Actions
Cell permeable: yes
Primary Target
EED (embryonic ectoderm development) - EZH2
EED (embryonic ectoderm development) - EZH2
Disclaimer
Toxicity: Standard Handling (A)
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.
Other Notes
Ac-FSSNRXKILXRTQILNQEWKQRRIQPV (X=(S)-2-(4ʹ-pentenyl)Ala, stapled)
Kim, W., et al. 2013. Nat. Chem. Biol.9, 643.
Packaging
Packaged under inert gas
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
常规特殊物品
此项目有
Kimberly H Kim et al.
Nature medicine, 22(2), 128-134 (2016-02-06)
Recent genomic studies have resulted in an emerging understanding of the role of chromatin regulators in the development of cancer. EZH2, a histone methyl transferase subunit of a Polycomb repressor complex, is recurrently mutated in several forms of cancer and
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