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203709 Insulin Expression Inducer, BRD7389 - CAS 376382-11-5 - Calbiochem

A cell-permeable naphthoquinolinedione compound that specifically induces insulin secretion in mouse αTC1-cells and promotes transdifferentiation to a β-cell-like status.

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Synonymes: 1-((2-Phenylethyl)amino)-3H-naphtho[1,2,3-de]quinoline-2,7-dione, Insulin Receptor-Related Protein Inhibitor, IRR Inhibitor, INSRR Inhibitor, RSK Inhibitor III

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203709
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Tableau de caractéristiques principal

CAS #Empirical Formula
376382-11-5C₂₄H₁₈N₂O₂

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      Description
      OverviewA cell-permeable naphthoquinolinedione compound that is reported to preferentially inhibit 23 kinases (IC50 ≤10 µM) from a panel of 219, notably IRR (h), CLK2(h), Rsk1(h), Flt3(h), Rsk1(r), Rsk2(h), Haspin(h), Rsk4(h), Melk(h), Drak1(h), Rsk3(h), and CK13(h) (% inhibition by 10 µM BRD7389 = 91, 87, 86, 79, 78, 76, 74, 73, 73, 72, 71, and 71, respectively). Shown to induce β-cell-like morphology in cultured murine pancreatic α-cell αTC1 and stimulate the expression of insulin mRNA (by ~50-fold; 0.85 µM for 5 d) and protein (by 1.5-fold; 3.4 µM for 5 d), as well as other β-cell mRNAs, including Iapp, Npy, Pdx1, and Pax4, in αTC1 cultures. In human primary islets cultures, BRD7389 treatments result in a decrease of overall cell counts over time due to apoptosis induction, while insulin-positive population, and in some cases also glucagon-positive cell population, remains more or less unaffected.
      Catalogue Number203709
      Brand Family Calbiochem®
      Synonyms1-((2-Phenylethyl)amino)-3H-naphtho[1,2,3-de]quinoline-2,7-dione, Insulin Receptor-Related Protein Inhibitor, IRR Inhibitor, INSRR Inhibitor, RSK Inhibitor III
      References
      ReferencesFomina-Yadlin, D., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 15099.
      Product Information
      CAS number376382-11-5
      FormOrange-yellow solid
      Hill FormulaC₂₄H₁₈N₂O₂
      Chemical formulaC₂₄H₁₈N₂O₂
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥98% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Regulatory Review
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing recontitution, 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
      Référence GTIN
      203709-10MG 04055977203790

      Documentation

      Insulin Expression Inducer, BRD7389 - CAS 376382-11-5 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Insulin Expression Inducer, BRD7389 - CAS 376382-11-5 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      203709

      Références bibliographiques

      Aperçu de la référence bibliographique
      Fomina-Yadlin, D., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 15099.
      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.

      Revision02-April-2012 JSW
      Synonyms1-((2-Phenylethyl)amino)-3H-naphtho[1,2,3-de]quinoline-2,7-dione, Insulin Receptor-Related Protein Inhibitor, IRR Inhibitor, INSRR Inhibitor, RSK Inhibitor III
      DescriptionA cell-permeable naphthoquinolinedione compound that is reported to preferentially inhibit 23 kinases (IC50 ≤10 µM) from a panel of 219, notably IRR (h), CLK2(h), Rsk1(h), Flt3(h), Rsk1(r), Rsk2(h), Haspin(h), Rsk4(h), Melk(h), Drak1(h), Rsk3(h), and CK13(h) (% inhibition by 10 µM BRD7389 = 91, 87, 86, 79, 78, 76, 74, 73, 73, 72, 71, and 71, respectively). Shown to induce β-cell-like morphology in cultured murine pancreatic α-cell αTC1 and stimulate the expression of insulin mRNA (by ~50-fold; 0.85 µM for 5 d) and protein (by 1.5-fold; 3.4 µM for 5 d), as well as other β-cell mRNAs, including Iapp, Npy, Pdx1, and Pax4, in αTC1 cultures. In human primary islets cultures, BRD7389 treatments result in a decrease of overall cell counts over time due to apoptosis induction, while insulin-positive population, and in some cases also glucagon-positive cell population, remains more or less unaffected.
      FormOrange-yellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number376382-11-5
      Chemical formulaC₂₄H₁₈N₂O₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing recontitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Toxicity Regulatory Review
      ReferencesFomina-Yadlin, D., et al. 2010. Proc. Natl. Acad. Sci. USA 107, 15099.