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

A cell-permeable, highly potent, ATP-competitive, reversible inhibitor of both GSK-3α and β (IC₅₀ = 650 and 580 pM, respectively).

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Synonymes: N²-(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

Primary Target: GSK-3 α & β
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531167
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Tableau de caractéristiques principal

CAS #Empirical Formula
252935-94-7C₂₀H₁₇Cl₂N₉O₂

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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
      Quality LevelMQ100
      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
      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
      Global Trade Item Number
      Référence GTIN
      5.31167.0001 04055977283150