508320 Ezh2 Inhibitor III, SAH-EZH2 - Calbiochem

508320
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₁₅₅H₂₅₆N₄₈O₄₀·6TFA·14H₂O

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      Glass bottle 2 mg
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      Description
      OverviewA 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; Kd = 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 Number508320
      Brand Family Calbiochem®
      SynonymsH3K27 Methylation Inhibitor, SAH-EZH2, EED-EZH2 Protein-Protein Interaction Inhibitor, SAH-EZH2, Enhancer of Zested Homolog 2 Inhibitor III, HMTase Inhibitor XIV
      References
      ReferencesKim, W., et al. 2013. Nat. Chem. Biol. 9, 643.
      Product Information
      FormWhite powder
      FormulationSupplied as a trifluoroacetate salt.
      Hill FormulaC₁₅₅H₂₅₆N₄₈O₄₀·6TFA·14H₂O
      Chemical formulaC₁₅₅H₂₅₆N₄₈O₄₀·6TFA·14H₂O
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetEED (embryonic ectoderm development) - EZH2
      Primary Target K<sub>i</sub>320 nM
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Peptide SequenceAc-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 InstructionsFollowing 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

      Documentation

      Ezh2 Inhibitor III, SAH-EZH2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Kim, W., et al. 2013. Nat. Chem. Biol. 9, 643.
      Data Sheet

      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.

      Revision28-March-2014 JSW
      SynonymsH3K27 Methylation Inhibitor, SAH-EZH2, EED-EZH2 Protein-Protein Interaction Inhibitor, SAH-EZH2, Enhancer of Zested Homolog 2 Inhibitor III, HMTase Inhibitor XIV
      DescriptionA 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; Kd = 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.
      FormWhite powder
      FormulationSupplied as a trifluoroacetate salt.
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₁₅₅H₂₅₆N₄₈O₄₀·6TFA·14H₂O
      Peptide SequenceAc-FSSNRXKILXRTQILNQEWKQRRIQPV (X=(S)-2-(4ʹ-pentenyl)Ala, stapled)
      Purity≥95% by HPLC
      SolubilityH₂O (100 mg/ml)
      Storage -20°C
      Protect from light
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesKim, W., et al. 2013. Nat. Chem. Biol. 9, 643.