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251635 Daminozide - CAS 1596-84-5 - Calbiochem

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251635
  
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      Overview

      Replacement Information
      Description
      OverviewA dimethylamino substituted succinamate that, in addition to its well known use as a plant growth regulator, also acts as an inhibitor against histone lysine demthylases KDM2A, LSD1 (KDM7A; KIAA1718), and PHF8 (IC50 = 1.5, 2.1, and 0.55 µM, respectively), but not KDM3A, KDM4E, KDM5C, KDM6B, or three hydroxylases (IC50 >100 µM). Substrate-competition and/or active site Iron chelating likely accounts for the inhibitory activity against the FAD-dependent LSD1, while 2-oxoglutarate (2-OG) competition (Ki = 1.97 µM) appears as the major mode of action against KDM2A.
      Catalogue Number251635
      Brand Family Calbiochem®
      SynonymsHistone Lysine Demethylase Inhibitor XII, LSD1 Inhibitor VI, N,N-Dimethylamino-succinamic acid, Succinic acid-2,2-dimethylhydrazide, 4-(2,2-Dimethylhydrazinyl)-4-oxobutanoic acid, BHC100 Inhibitor VI, KDM2A Inhibitor, KIAA1718 Inhibitor VI, LSD Inhibitor VI, PHF8 Inhibitor, JHDM Inhibitor VI
      References
      ReferencesRose, N.R., et al. 2012. J. Med. Chem. 55, 6639.
      Product Information
      CAS number1596-84-5
      FormWhite powder
      Hill FormulaC₆H₁₂N₂O₃
      Chemical formulaC₆H₁₂N₂O₃
      Hygroscopic Hygroscopic
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% by NMR
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      R PhraseR: 40

      Limited evidence of a carcinogenic effect.
      S PhraseS: 36/37/39

      Wear suitable protective clothing, gloves and eye/face protection.
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Harmful & Carcinogenic / Teratogenic
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      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
      Global Trade Item Number
      Catalog Number GTIN
      251635 0

      Documentation

      Daminozide - CAS 1596-84-5 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      Daminozide - CAS 1596-84-5 - Calbiochem Certificates of Analysis

      TitleLot Number
      251635

      References

      Reference overview
      Rose, N.R., et al. 2012. J. Med. Chem. 55, 6639.
      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.

      Revision11-April-2013 JSW
      SynonymsHistone Lysine Demethylase Inhibitor XII, LSD1 Inhibitor VI, N,N-Dimethylamino-succinamic acid, Succinic acid-2,2-dimethylhydrazide, 4-(2,2-Dimethylhydrazinyl)-4-oxobutanoic acid, BHC100 Inhibitor VI, KDM2A Inhibitor, KIAA1718 Inhibitor VI, LSD Inhibitor VI, PHF8 Inhibitor, JHDM Inhibitor VI
      DescriptionA dimethylamino substituted succinamic acid compound that, in addition to its well known use as a plant growth regulator, also acts as an inhibitor against histone lysine demthylases KDM2A, LSD1 (KDM7A; KIAA1718), and PHF8 (IC50 = 1.5, 2.1, and 0.55 µM, respectively), but not KDM3A, KDM4E, KDM5C, KDM6B, (IC50 >100 µM) or three hydroxylases (FIH, PHD2, and BBOX1; IC50 >100 µM). Although kinetic studies indicate 2-oxoglutarate (2-OG) competition (Ki = 1.97 µM) as the major mode of action against KDM2A, substrate-competition and/or active site Iron chelation more likely accounts for the compound's inhibitory activity against the FAD-dependent LSD1.
      FormWhite powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1596-84-5
      Chemical formulaC₆H₁₂N₂O₃
      Structure formulaStructure formula
      Purity≥98% by NMR
      SolubilityH₂O (10 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Hygroscopic
      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 & Carcinogenic / Teratogenic
      ReferencesRose, N.R., et al. 2012. J. Med. Chem. 55, 6639.