361571 InSolution™ GSK-3 Inhibitor XVI, CHIR99021 - CAS 252917-06-9 - Calbiochem

361571
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₂₂H₁₈Cl₂N₈252917-06-9

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361571-5MGCN
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      Glass bottle 5 mg
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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. The solid form of this compound (Cat. No. 361559) is also available.
      Catalogue Number361571
      Brand Family Calbiochem®
      Synonyms6-(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
      FormLiquid
      FormulationA 25 mM (5 mg/430 µL) solution of GSK-3 Inhibitor XVI, CHIR99021 (Cat. No. 361559) in DMSO.
      Hill FormulaC₂₂H₁₈Cl₂N₈
      Hygroscopic Hygroscopic
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetGSK-3 α and β
      Primary Target IC<sub>50</sub>10 and 6.7 nM against GSK-3&alpha
      Purity≥90% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      R PhraseR: 36/38

      Irritating to eyes 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 Dry Ice Only
      Toxicity Irritant
      Storage ≤ -70°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Avoid freeze/thaw Avoid freeze/thaw
      Do not freeze Ok to freeze
      Special InstructionsFollowing initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      InSolution™ GSK-3 Inhibitor XVI, CHIR99021 - CAS 252917-06-9 - Calbiochem Certificates of Analysis

      TitleLot Number
      361571

      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.

      Revision13-July-2020 JSW
      Synonyms6-(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). 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. The solid form of this compound (Cat. No. 361559) is also available.
      FormLiquid
      FormulationA 25 mM (5 mg/430 µL) solution of GSK-3 Inhibitor XVI, CHIR99021 (Cat. No. 361559) in DMSO.
      Intert gas (Yes/No) Packaged under inert gas
      CAS number252917-06-9
      Structure formulaStructure formula
      Purity≥90% by HPLC
      Storage ≤ -70°C
      Hygroscopic
      Protect from light
      Avoid freeze/thaw
      Do Not Freeze Ok to freeze
      Special InstructionsFollowing initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.
      Toxicity Irritant
      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.