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217531 CARM1 Inhibitor - CAS 1020399-49-8 - Calbiochem

The CARM1 Inhibitor controls the biological activity of CARM1. This small molecule/inhibitor is primarily used for Cell Structure applications.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: PRMT Inhibitor V, Coactivator-Associated Arginine Methyltransferase 1 Inhibitor, 1-Benzyl-3,5-bis-(3-bromo-4-hydroxybenzylidene)piperidin-4-one, 3,5-bis(3-Bromo-4-hydroxybenzylidene)-1-benzylpiperidin-4-one

Primary Target: PRMT4
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217531
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Tableau de caractéristiques principal

CAS #Empirical Formula
1020399-49-8C₂₆H₂₁Br₂NO₃

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217531-10MG
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      Description
      OverviewA cell-permeable (bis-benzylidene)piperidinone compound that acts as a selective inhibitor against CARM1/PRMT4 arginine methyltransferase activity (IC50 = 7.1 µM with PABP1 as substrate). It inhibits PRMT3 only at much higher concentrations (by 70% and 62% with 100 µM inhibitor using NPL3 or rpS2 as substrate, respectively), exhibiting little activity against PRMT1, PRMT5, PRMT6 (IC50 >100 µM), or four HKMTs (<20% inhibition against DOTL1, G9a, SET7, or Suv39H1 with 100 µM inhibitor). Shown to inhibit PSA promoter-mediated reporter transcription in LNCaP cells in a dose-dependent manner (by 74% and 97%, respectively, with 4 and 6 µM inhibitor).
      Catalogue Number217531
      Brand Family Calbiochem®
      SynonymsPRMT Inhibitor V, Coactivator-Associated Arginine Methyltransferase 1 Inhibitor, 1-Benzyl-3,5-bis-(3-bromo-4-hydroxybenzylidene)piperidin-4-one, 3,5-bis(3-Bromo-4-hydroxybenzylidene)-1-benzylpiperidin-4-one
      References
      ReferencesCheng, D., et al. 2011. J. Med. Chem. 54, 4928.
      Product Information
      CAS number1020399-49-8
      FormOrange solid
      Hill FormulaC₂₆H₂₁Br₂NO₃
      Chemical formulaC₂₆H₂₁Br₂NO₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPRMT4
      Primary Target IC<sub>50</sub>CARM1-mediated methylation over PRMT1 and SET7 (IC₅₀ = 7.1, 63 and 943 µM,
      Secondary targetSET7
      Purity≥95% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°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
      Global Trade Item Number
      Référence GTIN
      217531-10MG 04055977219388

      Documentation

      CARM1 Inhibitor - CAS 1020399-49-8 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      CARM1 Inhibitor - CAS 1020399-49-8 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      217531

      Références bibliographiques

      Aperçu de la référence bibliographique
      Cheng, D., et al. 2011. J. Med. Chem. 54, 4928.
      Fiche technique

      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.

      Revision18-July-2012 JSW
      SynonymsPRMT Inhibitor V, Coactivator-Associated Arginine Methyltransferase 1 Inhibitor, 1-Benzyl-3,5-bis-(3-bromo-4-hydroxybenzylidene)piperidin-4-one, 3,5-bis(3-Bromo-4-hydroxybenzylidene)-1-benzylpiperidin-4-one
      DescriptionA cell-permeable (bis-benzylidene)piperidinone compound that acts as a selective inhibitor against CARM1/PRMT4 arginine methyltransferase activity (IC50 = 7.1 µM with PABP1 as substrate). It inhibits PRMT3 only at much higher concentrations (by 70% and 62% with 100 µM inhibitor using NPL3 or rpS2 as substrate, respectively), exhibiting little activity against PRMT1, PRMT5, PRMT6 (IC50 >100 µM), or four HKMTs (<20% inhibition against DOTL1, G9a, SET7, or Suv39H1 with 100 µM inhibitor). Shown to inhibit PSA promoter-mediated reporter transcription in LNCaP cells in a dose-dependent manner (by 74% and 97%, respectively, with 4 and 6 µM inhibitor).
      FormOrange solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1020399-49-8
      Chemical formulaC₂₆H₂₁Br₂NO₃
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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
      ReferencesCheng, D., et al. 2011. J. Med. Chem. 54, 4928.