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

361571
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₂H₁₈Cl₂N₈ 252917-06-9

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      361571-5MG
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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
          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≥95% 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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.

          Revision21-September-2012 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≥95% 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.