382191 | HMTase Inhibitor II, Chaetocin - CAS 28097-03-2 - Calbiochem

382191
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₃₀H₂₈N₆O₆S₄ 28097-03-2

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      382191-500UG
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          Plastic ampoule 500 μg
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          Description
          OverviewA naturally occurring cell-permeable Chaetomium fungal epi-dithio-diketopiperazine that potently inhibits the H3K9 histone methyltransferase activity of Drosophila melanogaster SU(VAR)3-9 and its human homologue SUV39H1 (IC50 = 600 and 800 nM, respectively) in a SAM-competitive manner, while exhibiting much reduced potency against murine G9a or Neurospora crassa DIM5 H3K9 HMT (IC50 = 2.5 and 3 µM, respectively) and no activity against the H3K27 HMTase activity of Drosophila E(z), the H3K4 activity of bacterial SET7/9, or the H4K20 activity of bacterial PRSET7. Although the reduction of intramolecular disulfide bonds of Chaetocin does not affect its HMTase inhibitory activity in cell-free enzymatic assays, the integrity of the disulfide bonds is shown to be essential for its cellular uptake. Myeloma cell lines as well as myeloma cells isolated from patients are shown to be especially susceptible to death upon H2O2 or Chaetocin treatment due to their heightened sensitivity to cellular oxidative stress induced by these agents.
          Catalogue Number382191
          Brand Family Calbiochem®
          SynonymsHMT Inhibitor II, Histone Lysine Methyltransferase Inhibitor II, EHMT2/G9a Inhibitor II
          References
          ReferencesIsham, C.R., et al. 2007. Blood 109, 2579.
          Greiner, D., et al. 2005. Nat. Chem. Biol. 1, 143.
          Product Information
          CAS number28097-03-2
          FormWhite to off-white solid
          Hill FormulaC₃₀H₂₈N₆O₆S₄
          Chemical formulaC₃₀H₂₈N₆O₆S₄
          Structure formula ImageStructure formula Image
          Applications
          Biological Information
          Purity≥97% by HPLC
          Physicochemical Information
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          R PhraseR: 20/21/22

          Harmful by inhalation, in contact with skin and if swallowed.
          S PhraseS: 22-26-36-45

          Do not breathe dust.
          In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
          Wear suitable protective clothing.
          In case of accident or if you feel unwell, seek medical advice immediately (show the label where possible).
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Harmful
          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 6 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) 

          Certificates of Analysis

          TitleLot Number
          382191

          References

          Reference overview
          Isham, C.R., et al. 2007. Blood 109, 2579.
          Greiner, D., et al. 2005. Nat. Chem. Biol. 1, 143.

          Technical Info

          Title
          White Paper - The Message in the Marks: Deciphering Cancer Epigenetics (EMD)
          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.

          Revision23-March-2018 JSW
          SynonymsHMT Inhibitor II, Histone Lysine Methyltransferase Inhibitor II, EHMT2/G9a Inhibitor II
          DescriptionA naturally occurring cell-permeable Chaetomium fungal epi-dithio-diketopiperazine that potently inhibits the H3K9 histone methyltransferase activity of Drosophila melanogaster SU(VAR)3-9 and its human homologue SUV39H1 (IC50 = 600 and 800 nM, respectively) in a SAM-competitive manner, while exhibiting much reduced potency against murine G9a or Neurospora crassa DIM5 H3K9 HMT (IC50 = 2.5 and 3 µM, respectively) and no activity against the H3K27 HMTase activity of Drosophila E(z), the H3K4 activity of bacterial SET7/9, or the H4K20 activity of bacterial PRSET7. Although the reduction of intramolecular disulfide bonds of Chaetocin does not affect its HMTase inhibitory activity in cell-free enzymatic assays, the integrity of the disulfide bonds is shown to be essential for its cellular uptake. Myeloma cell lines as well as myeloma cells isolated from patients are shown to be especially susceptible to death upon H2O2 or Chaetocin treatment due to their heightened sensitivity to cellular oxidative stress induced by these agents.
          FormWhite to off-white solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number28097-03-2
          Chemical formulaC₃₀H₂₈N₆O₆S₄
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (1 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 6 months at -20°C.
          Toxicity Harmful
          ReferencesIsham, C.R., et al. 2007. Blood 109, 2579.
          Greiner, D., et al. 2005. Nat. Chem. Biol. 1, 143.