382193 HMTase Inhibitor V, UNC0224 - CAS 1197196-48-7 - Calbiochem

382193
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₆H₄₃N₇O₂ • H₂O 1197196-48-7

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      382193-5MG
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          Glass bottle 5 mg
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          Description
          OverviewA quinazolinamine compound that inhibits G9a and GLP histone H3K9 methyltransferase activity (IC50 ~50 and 54 nM, respectively) by targeting the lysine binding channel, while affecting muscarinic M2 receptor and histamine H1 receptor only at much higher concentrations (by 82% and 31%, respectively, at 1 µM) and exhibiting little activity against SET7/9, SET8/PreSET7, PRMT3, JMJD2E (IC50 >40 µM), or a panel of 30 GPCR, ion channels, and transporters (<20% inhibition at 1 µM).
          Catalogue Number382193
          Brand Family Calbiochem®
          Synonyms7-(3-Dimethylaminopropoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine, H₂O, Histone Lysine Methyltransferase Inhibitor V, UNC0224, EHMT1/GLP Inhibitor III, EHMT2/G9a Inhibitor V
          References
          ReferencesLiu, F., et al. 2010. J. Med. Chem. 53, 5844.
          Liu, F., et al. 2009. J. Med. Chem. 52, 7950.
          Product Information
          CAS number1197196-48-7
          FormLiquid
          Hill FormulaC₂₆H₄₃N₇O₂ • H₂O
          Chemical formulaC₂₆H₄₃N₇O₂ • H₂O
          Hygroscopic Hygroscopic
          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
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Dry Ice Only
          Toxicity Standard Handling
          Storage ≤ -70°C
          Protect from Light Protect from light
          Hygroscopic Hygroscopic
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°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
          Liu, F., et al. 2010. J. Med. Chem. 53, 5844.
          Liu, F., et al. 2009. J. Med. Chem. 52, 7950.
          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.

          Revision26-March-2012 JSW
          Synonyms7-(3-Dimethylaminopropoxy)-6-methoxy-2-(4-methyl-1,4-diazepan-1-yl)-N-(1-methylpiperidin-4-yl)quinazolin-4-amine, H₂O, Histone Lysine Methyltransferase Inhibitor V, UNC0224, EHMT1/GLP Inhibitor III, EHMT2/G9a Inhibitor V
          DescriptionA quinazolinamine compound that acts as a highly potent inhibitor against G9a (IC50 = 43 and 57 nM by SAHH production determination/ECSD and substrate lysine methylation detection/CLOT, respectively) and GLP (IC50 = 50 and 58 nM by ECSD and CLOT, respectively) histone H3K9 methyltransferase activity, while affecting muscarinic M2 receptor and histamine H1 receptor only at much higher concentrations (by 82% and 31%, respectively, at 1 µM) and exhibiting little activity against SET7/9, SET8/PreSET7, PRMT3, JMJD2E (IC50 >40 µM), or a panel of 30 GPCR, ion channels, and transporters (<20% inhibition at 1 µM). X-ray crystallography study reveals that UNC0224 exerts its inhibition by occupying G9a lysine binding channel via its 7-dimethylamino propoxy side chain.
          FormLiquid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number1197196-48-7
          Chemical formulaC₂₆H₄₃N₇O₂ • H₂O
          Structure formulaStructure formula
          Purity≥97% by HPLC
          SolubilityDMSO (100 mg/ml)
          Storage ≤ -70°C
          Hygroscopic
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
          Toxicity Standard Handling
          ReferencesLiu, F., et al. 2010. J. Med. Chem. 53, 5844.
          Liu, F., et al. 2009. J. Med. Chem. 52, 7950.