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361559 GSK-3 Inhibitor XVI - CAS 252917-06-9 - Calbiochem

GSK-3 Inhibitor XVI - CAS 252917-06-9, is a cell-permeable, potent, ATP-competitive, and highly selective GSK-3 inhibitor (IC₅₀ = 10 and 6.7 nM against GSK-3α and GSK-3β, respectively).

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

Synonyms: CHIR99021, 6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile

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361559
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
252917-06-9C₂₂H₁₈Cl₂N₈

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      Description
      OverviewA cell-permeable aminopyrimidine compound that acts as potent, ATP-competitive, and highly selective GSK-3 inhibitor (IC50 = 10 and 6.7 nM against GSK-3α and GSK-3β, respectively). Exhibits little or no activity toward 46 other enzymes (IC50 >8.8 µM against 20 kinases and Ki ≥5 µM against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (Kd ~4 µM). This compound is orally available and is shown to effectively improve glucose metabolism in both murine and rat type 2 diabetes models in vivo. Also available as a 25 mM solution in DMSO (Cat. No. 361571).
      Catalogue Number361559
      Brand Family Calbiochem®
      SynonymsCHIR99021, 6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile
      References
      ReferencesMussmann, R., et al. 2007. J. Biol. Chem. 282, 12030.
      Ring, D.B., et al. 2003. Diabetes 52, 588.
      Bennett, C.N., et al. 2002. J. Biol. Chem. 277, 30998.
      Cline, G.W., et al. 2002. Diabetes 51, 2903.
      Product Information
      CAS number252917-06-9
      FormWhite to beige solid
      Hill FormulaC₂₂H₁₈Cl₂N₈
      Chemical formulaC₂₂H₁₈Cl₂N₈
      Structure formula ImageStructure formula Image
      Quality LevelMQ200
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      R PhraseR: 22

      Harmful if swallowed.
      S PhraseS: 22-24/25-36-45

      Do not breathe dust.
      Avoid contact with skin and eyes.
      Wear suitable protective clothing.
      In case of accident or if you feel unwell, seek medical advice immediately (show the label where possible).
      Product Usage Statements
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Harmful
      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 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
      361559-5MG 04055977214208

      Documentation

      GSK-3 Inhibitor XVI - CAS 252917-06-9 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      GSK-3 Inhibitor XVI - CAS 252917-06-9 - Calbiochem Certificates of Analysis

      TitleLot Number
      361559

      References

      Reference overview
      Mussmann, R., et al. 2007. J. Biol. Chem. 282, 12030.
      Ring, D.B., et al. 2003. Diabetes 52, 588.
      Bennett, C.N., et al. 2002. J. Biol. Chem. 277, 30998.
      Cline, G.W., et al. 2002. Diabetes 51, 2903.
      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.

      Revision18-June-2020 JSW
      SynonymsCHIR99021, 6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile
      DescriptionA cell-permeable aminopyrimidine compound that acts as potent, ATP-competitive, and highly selective GSK-3 inhibitor (IC50 = 10 and 6.7 nM against GSK-3α and GSK-3β, respectively). CHIR99021 exhibits little or no activity toward 46 other enzymes (IC50 >8.8 µM against 20 kinases and Ki ≥5 µM against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (Kd ~4 µM). CHIR99021 is orally available and is shown to effectively improve glucose metabolism in both murine and rat type 2 diabetes models in vivo.
      FormWhite to beige solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number252917-06-9
      Chemical formulaC₂₂H₁₈Cl₂N₈
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (5 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 6 months at -20°C.
      Toxicity Harmful
      ReferencesMussmann, R., et al. 2007. J. Biol. Chem. 282, 12030.
      Ring, D.B., et al. 2003. Diabetes 52, 588.
      Bennett, C.N., et al. 2002. J. Biol. Chem. 277, 30998.
      Cline, G.W., et al. 2002. Diabetes 51, 2903.