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508320 Sigma-AldrichEzh2 Inhibitor III, SAH-EZH2 - Calbiochem

A helical 27-mer peptide with E54Q modification that directly binds to EDD (Kd = 320 nM) and disrupts protein-protein interaction of EED with EZH2 and EZH1.

Ezh2 Inhibitor III, SAH-EZH2 - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
参考
Data Sheet

同义词: H3K27 Methylation Inhibitor, SAH-EZH2, EED-EZH2 Protein-Protein Interaction Inhibitor, SAH-EZH2, Enhancer of Zested Homolog 2 Inhibitor III, HMTase Inhibitor XIV

Primary Target: EED (embryonic ectoderm development) - EZH2

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概述

Replacement Information

重要规格表

Empirical Formula
C₁₅₅H₂₅₆N₄₈O₄₀·6CF₃CO₂H·XXH₂O

价格及供货情况

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Description
Overview	A stabilized a-helical 27-mer peptide (FSSNRXKILXRTQILNQEWKQRRIQPV) with E54Q modification that exhibits robust cellular uptake and nuclear localization and directly binds to embryonic ectoderm development (EED; K_d = 320 nM) and disrupts protein-protein interaction of EED with EZH2 ( Enhancer of zeste homolog 2 ) and EZH1. Selectively inhibits methyltransferase activity of the Polycomb repressive complex 2 (PRC2) and reduces H3K27 methylation in a dose-dependent manner (~1 to 10 µM). Induces growth arrest at the Go/G1 phase (after 6 days of treatment) and monocyte-macrophage differentiation in MLL-AF9 leukemia cells without inducing any apoptosis. Growth arrest is suggested to be associated with an increase in p19ARF levels. Shown to block the proliferation of C1498 and M1 myeloid leukemia cells without affecting non-tumorigenic HPC5 cells. Please note that the molecular weight for this compound is batch-specific due to variable water content.
Catalogue Number	508320
Brand Family	Calbiochem®
Synonyms	H3K27 Methylation Inhibitor, SAH-EZH2, EED-EZH2 Protein-Protein Interaction Inhibitor, SAH-EZH2, Enhancer of Zested Homolog 2 Inhibitor III, HMTase Inhibitor XIV

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

Product Information
Form	White powder
Formulation	Supplied as a trifluoroacetate salt.
Hill Formula	C₁₅₅H₂₅₆N₄₈O₄₀·6CF₃CO₂H·XXH₂O
Chemical formula	C₁₅₅H₂₅₆N₄₈O₄₀·6CF₃CO₂H·XXH₂O
Quality Level	MQ100

Applications

Biological Information
Primary Target	EED (embryonic ectoderm development) - EZH2
Primary Target K<sub>i</sub>	320 nM
Purity	≥95% by HPLC

Physicochemical Information
Cell permeable	Y
Peptide Sequence	Ac-FSSNRXKILXRTQILNQEWKQRRIQPV (X=(S)-2-(4ʹ-pentenyl)Ala, stapled)

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Shipped with Blue Ice or with Dry Ice
Toxicity	Standard Handling
Storage	-20°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
5.08320.0001	04055977261882

Documentation

Ezh2 Inhibitor III, SAH-EZH2 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

参考

参考信息概述
Kim, W., et al. 2013. Nat. Chem. Biol. 9, 643.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	28-March-2014 JSW
Synonyms	H3K27 Methylation Inhibitor, SAH-EZH2, EED-EZH2 Protein-Protein Interaction Inhibitor, SAH-EZH2, Enhancer of Zested Homolog 2 Inhibitor III, HMTase Inhibitor XIV
Description	A stabilized a-helical 27-mer peptide (FSSNRXKILXRTQILNQEWKQRRIQPV) with E54Q modification that exhibits robust cellular uptake and nuclear localization and directly binds to embryonic ectoderm development (EED; K_d = 320 nM) and disrupts protein-protein interaction of EED with EZH2 ( Enhancer of zeste homolog 2 ) and EZH1. Selectively inhibits methyltransferase activity of the Polycomb repressive complex 2 (PRC2) and reduces H3K27 methylation in a dose-dependent manner (~1 to 10 µM). Induces growth arrest at the Go/G1 phase (after 6 days of treatment) and monocyte-macrophage differentiation in MLL-AF9 leukemia cells without inducing any apoptosis. Growth arrest is suggested to be associated with an increase in p19ARF levels. Shown to block the proliferation of C1498 and M1 myeloid leukemia cells without affecting non-tumorigenic HPC5 cells.
Form	White powder
Formulation	Supplied as a trifluoroacetate salt.
Intert gas (Yes/No)	Packaged under inert gas
Chemical formula	C₁₅₅H₂₅₆N₄₈O₄₀·6CF₃CO₂H·XXH₂O
Peptide Sequence	Ac-FSSNRXKILXRTQILNQEWKQRRIQPV (X=(S)-2-(4ʹ-pentenyl)Ala, stapled)
Purity	≥95% by HPLC
Solubility	H₂O (100 mg/ml)
Storage	Protect from light -20°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Toxicity	Standard Handling
References	Kim, W., et al. 2013. Nat. Chem. Biol. 9, 643.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Cell Cycle/Cell Division > Histone Acetylase and Deacetylase Inhibitors

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