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

361566
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₉H₁₂Cl₂N₂O₂ 280744-09-4

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      361566-10MG
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          Glass bottle 10 mg
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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
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.