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

382193
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Key Specifications Table

Empirical FormulaCAS #
C₂₆H₄₃N₇O₂ • H₂O 1197196-48-7

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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
      Quality LevelMQ100
      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

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

      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.

      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.