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531167 | GSK-3 Inhibitor XXIX, CHIR98014 - CAS 252935-94-7 - Calbiochem

531167
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₀H₁₇Cl₂N₉O₂ 252935-94-7

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      5311670001
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          Glass bottle 5 mg
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          Description
          OverviewA cell-permeable, brain permeant aminopyrimidine compound that acts as a potent, ATP-competitive and reversible inhibitor of both GSK-3α and β (IC50 = 650 and 580 pM, respectively; Ki = 870 pM for human GSK-3β) and significantly affects downstream effects of GSK-3. Displays excellent selectivity over closely related Cdc2 and Erk2 (IC50 = 3.7 µM & > 10 µM, respectively). Does not affect the activity of several other protein kinases studied. Acutely sensitizes glycogen synthase activity in isolated skeletal muscle from insulin-sensitive lean Zucker and insulin-resistant Zucker diabetic fatty (ZDF) rats and can also augment insulin-stimulated glucose uptake in ZDF rats. However, it does not affect the basal glucose uptake rate. Induces a significant reduction in fasting hyperglycemia in diabetic and insulin-resistant db/db mice (~30 mg/kg, s.c.). Reduces Tau phosphorylation (Ser396) in the cortex and hippocampus of postnatal rats. Also shown to activate Wnt/β-catenin signaling and direct the differentiation of human pluripotent stem cells into cardiomyocytes.

          Please note that the molecular weight for this compound is batch-specific due to variable water content.
          Catalogue Number531167
          Brand Family Calbiochem®
          SynonymsN²-(2-(4-(2,4-Dichlorophenyl)-5-(1H-imidazol-1-yl)pyrimidin-2-ylamino)ethyl)-5-nitropyridine-2,6-diamine, N⁶-(2-((4-(2,4-Dichlorophenyl)-5-(1H-imidazol-1-yl)-2-pyrimidinyl)amino}ethyl)-3-nitro-2,6-pyridinediamine, CHIR-98014, CT-98014
          References
          ReferencesGrigoryan, T., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 18174.
          Lian, X., et al. 2012. Proc. Natl. Acad. Sci. USA 109, E1848.
          Selenica, M.L., et al. 2007. Br. J. Pharmacol. 152, 959.
          Ring, D.B., et al. 2003. Diabetes. 52, 588.
          Nikoulina, S.E., et al. 2002. Diabetes. 51, 2190.
          Product Information
          CAS number252935-94-7
          FormYellow powder
          Hill FormulaC₂₀H₁₇Cl₂N₉O₂
          Chemical formulaC₂₀H₁₇Cl₂N₉O₂
          ReversibleY
          Applications
          Biological Information
          Primary TargetGSK-3 α & β
          Primary Target IC<sub>50</sub>650 and 580 pM for GSK-3&alpha
          Primary Target K<sub>i</sub>870 pM for human GSK-3&beta
          Purity≥95% by HPLC
          Physicochemical Information
          Cell permeableY
          Dimensions
          Materials Information
          Toxicological Information
          Safety Information according to GHS
          Safety Information
          Product Usage Statements
          Storage and Shipping Information
          Ship Code Ambient Temperature Only
          Toxicity Standard Handling
          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

          Documentation

          References

          Reference overview
          Grigoryan, T., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 18174.
          Lian, X., et al. 2012. Proc. Natl. Acad. Sci. USA 109, E1848.
          Selenica, M.L., et al. 2007. Br. J. Pharmacol. 152, 959.
          Ring, D.B., et al. 2003. Diabetes. 52, 588.
          Nikoulina, S.E., et al. 2002. Diabetes. 51, 2190.

          Technical Info

          Title
          White Paper: Further considerations of antibody validation and usage. (EMD)
          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.

          Revision27-March-2015 JSW
          SynonymsN²-(2-(4-(2,4-Dichlorophenyl)-5-(1H-imidazol-1-yl)pyrimidin-2-ylamino)ethyl)-5-nitropyridine-2,6-diamine, N⁶-(2-((4-(2,4-Dichlorophenyl)-5-(1H-imidazol-1-yl)-2-pyrimidinyl)amino}ethyl)-3-nitro-2,6-pyridinediamine, CHIR-98014, CT-98014
          DescriptionA cell-permeable, brain permeant aminopyrimidine compound that acts as a potent, ATP-competitive and reversible inhibitor of both GSK-3α and β (IC50 = 650 and 580 pM, respectively; Ki = 870 pM for human GSK-3β) and significantly affects downstream effects of GSK-3. Displays excellent selectivity over closely related Cdc2 and Erk2 (IC50 = 3.7 µM & > 10 µM, respectively). Does not affect the activity of several other protein kinases studied. Acutely sensitizes glycogen synthase activity in isolated skeletal muscle from insulin-sensitive lean Zucker and insulin-resistant Zucker diabetic fatty (ZDF) rats and can also augment insulin-stimulated glucose uptake in ZDF rats. However, it does not affect the basal glucose uptake rate. Induces a significant reduction in fasting hyperglycemia in diabetic and insulin-resistant db/db mice (~30 mg/kg, s.c.). Reduces Tau phosphorylation (Ser396) in the cortex and hippocampus of postnatal rats. Also shown to activate Wnt/β-catenin signaling and direct the differentiation of human pluripotent stem cells into cardiomyocytes.
          FormYellow powder
          Intert gas (Yes/No) Packaged under inert gas
          CAS number252935-94-7
          Chemical formulaC₂₀H₁₇Cl₂N₉O₂
          Purity≥95% by HPLC
          SolubilityDMSO (25 mg/ml)
          Storage +2°C to +8°C
          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.
          Toxicity Standard Handling
          ReferencesGrigoryan, T., et al. 2013. Proc. Natl. Acad. Sci. USA 110, 18174.
          Lian, X., et al. 2012. Proc. Natl. Acad. Sci. USA 109, E1848.
          Selenica, M.L., et al. 2007. Br. J. Pharmacol. 152, 959.
          Ring, D.B., et al. 2003. Diabetes. 52, 588.
          Nikoulina, S.E., et al. 2002. Diabetes. 51, 2190.