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361566 GSK-3 Inhibitor IV, SB-216763 - CAS 280744-09-4 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: SB-216763

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361566
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
280744-09-4C₁₉H₁₂Cl₂N₂O₂

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      Description
      OverviewA cell-permeable (aryl,indole) maleimide compound that acts as a potent, selective, ATP-competitive inhibitor of GSK-3 activity (Ki = 9.1 nM for GSK-3α). At 10 µM concentration, does not significantly inhibit a panel of 24 other protein kinases tested. Reported to stimulate glycogen synthesis in Chang human liver cells (EC50 = 3.6 µM) and induce transcription of β-catenin-LEF/TCF (lymphoid enhancer factor/T cell factor) regulated reporter gene in HEK293 human embryonic kidney cell lines. Offers protection against polyglutamine-induced death in SK-N-SH and COS-7 cells and attenuates hypoxia-induced apoptosis in VSMC and COS-7 cells. Shown to reduce phosphoenolpyruvate carboxykinase (PEPCK) and glucose-6-phosphatase (G6Pase) expression in hepatoma cells. Promotes the survival of CLL lymphocytes via Wnt/β-catenin-mediated transcription activation. Exhibits delayed cardioprotection in vivo in a rat model via a KATP (ATP-sensitive potassium channels) and MPTP (mitochondrial permeability transition pore)-dependent mechanism at reperfusion.
      Catalogue Number361566
      Brand Family Calbiochem®
      SynonymsSB-216763
      References
      ReferencesGross, E., et al. 2008. Am. J. Phy. Heart Circ Physiol. 294, H1497.
      Bain, J., et al. 2007. Biochem. J. 408, 297.
      Lu, D., et al. 2004. PNAS. 101, 3118.
      Carmichael, J., et al. 2002. J. Biol. Chem. 277, 33791.
      Culbert, A.A., et al. 2001. FEBS Lett. 507, 288.
      Lochhead, P.A., et al. 2001. Diabetes 50, 937.
      Cross, D.A., et al. 2001. J. Neurochem. 77, 94.
      Coghlan, M.P., et al. 2000. Chem. Biol. 7, 793.
      Product Information
      CAS number280744-09-4
      FormOrange solid
      Hill FormulaC₁₉H₁₂Cl₂N₂O₂
      Chemical formulaC₁₉H₁₂Cl₂N₂O₂
      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
      R PhraseR: 36/37/38

      Irritating to eyes, respiratory system and skin.
      S PhraseS: 26-36

      In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
      Wear suitable protective clothing.
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Irritant
      Storage +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.
      Packaging Information
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      361566-10MG 04055977214246

      Documentation

      GSK-3 Inhibitor IV, SB-216763 - CAS 280744-09-4 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      GSK-3 Inhibitor IV, SB-216763 - CAS 280744-09-4 - Calbiochem Certificates of Analysis

      TitleLot Number
      361566

      References

      Reference overview
      Gross, E., et al. 2008. Am. J. Phy. Heart Circ Physiol. 294, H1497.
      Bain, J., et al. 2007. Biochem. J. 408, 297.
      Lu, D., et al. 2004. PNAS. 101, 3118.
      Carmichael, J., et al. 2002. J. Biol. Chem. 277, 33791.
      Culbert, A.A., et al. 2001. FEBS Lett. 507, 288.
      Lochhead, P.A., et al. 2001. Diabetes 50, 937.
      Cross, D.A., et al. 2001. J. Neurochem. 77, 94.
      Coghlan, M.P., et al. 2000. Chem. Biol. 7, 793.
      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.

      Revision14-August-2012 JSW
      SynonymsSB-216763
      DescriptionA cell-permeable (aryl,indole) maleimide compound that acts as a potent, selective, ATP-competitive inhibitor of GSK-3 activity (Ki = 9.1 nM for GSK-3α). At 10 µM concentration, does not significantly inhibit a panel of 24 other protein kinases tested. Reported to stimulate glycogen synthesis in Chang human liver cells (EC50 = 3.6 µM) and induce transcription of β-catenin-LEF/TCF (lymphoid enhancer factor/T cell factor) regulated reporter gene in HEK293 human embryonic kidney cell lines. Offers protection against polyglutamine-induced death in SK-N-SH and COS-7 cells and attenuates hypoxia-induced apoptosis in VSMC and COS-7 cells. Shown to reduce phosphoenolpyruvate carboxykinase (PEPCK) and glucose-6-phosphatase (G6Pase) expression in hepatoma cells. Promotes the survival of CLL lymphocytes via Wnt/β-catenin-mediated transcription activation. Exhibits delayed cardioprotection in vivo in a rat model via a KATP (ATP-sensitive potassium channels) and MPTP (mitochondrial permeability transition pore)-dependent mechanism at reperfusion.
      FormOrange solid
      CAS number280744-09-4
      Chemical formulaC₁₉H₁₂Cl₂N₂O₂
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage +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 Irritant
      ReferencesGross, E., et al. 2008. Am. J. Phy. Heart Circ Physiol. 294, H1497.
      Bain, J., et al. 2007. Biochem. J. 408, 297.
      Lu, D., et al. 2004. PNAS. 101, 3118.
      Carmichael, J., et al. 2002. J. Biol. Chem. 277, 33791.
      Culbert, A.A., et al. 2001. FEBS Lett. 507, 288.
      Lochhead, P.A., et al. 2001. Diabetes 50, 937.
      Cross, D.A., et al. 2001. J. Neurochem. 77, 94.
      Coghlan, M.P., et al. 2000. Chem. Biol. 7, 793.