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About This Item
Empirical Formula (Hill Notation):
C155H256N48O40 · 6CF3CO2H · XXH2O
UNSPSC Code:
12352200
NACRES:
NA.77
Assay
≥95% (HPLC)
Quality Level
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
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
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
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
Flash Point(F)
Not applicable
Flash Point(C)
Not applicable
Certificates of Analysis (COA)
Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.
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