508320 Ezh2 Inhibitor III, SAH-EZH2 - Calbiochem

508320
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₁₅₅H₂₅₆N₄₈O₄₀·6TFA·14H₂O

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.08320.0001
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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
          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

          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.