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361569 GSK-3beta Inhibitor XXVI - Calbiochem

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361569
  
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₂₁H₁₈N₄O
      Description
      Overview

      This product has been discontinued.



      A cell-permeable, pyrazolone GSK-3β inhibitor (IC50 = 34 nM, in an enzymatic assay) that is highly selective among a panel of 40 kinases that have been profiled with more than 50 fold selectivity. It exhibits no off-target activity against a panel of 44 human and rodent CNS receptors, channels, and transporters except for some modest activity toward 5HT1a. It demonstrates neuroprotective activity of neurons in an oxidative stress model induced by homocysteic acid (HCA) from 1–20 µM, without observable cytotoxicity, and is superior to SB-216763 Cat. No. 361566) at 5 µM in cell micrographs. In addition, it is shown to attenuate locomotor activity in an chlordiazepoxide/amphetamine-induced hyperactivity mice model in vivo at 150 mg/kg.

      Catalogue Number361569
      Brand Family Calbiochem®
      References
      ReferencesChen, W., et al. 2011. ChemMedChem 6, 1587.
      Product Information
      FormWhite solid
      Hill FormulaC₂₁H₁₈N₄O
      Chemical formulaC₂₁H₁₈N₄O
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥95% by HPLC
      Physicochemical Information
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Catalogue Number GTIN
      361569 0

      Documentation

      GSK-3beta Inhibitor XXVI - Calbiochem Certificates of Analysis

      TitleLot Number
      361569

      References

      Reference overview
      Chen, W., et al. 2011. ChemMedChem 6, 1587.
      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.

      Revision26-April-2012 JSW
      DescriptionA cell-permeable, pyrazolone GSK-3β inhibitor (IC50 = 34 nM, in an enzymatic assay) that is highly selective among a panel of 40 kinases that have been profiled with more than 50 fold selectivity. It exhibits no off-target activity against a panel of 44 human and rodent CNS receptors, channels, and transporters except for some modest activity toward 5HT1a. It demonstrates neuroprotective activity of neurons in an oxidative stress model induced by homocysteic acid (HCA) from 1–20 µM, without observable cytotoxicity, and is superior to SB-216763 Cat. No. 361566) at 5 µM in cell micrographs. In addition, it is shown to attenuate locomotor activity in an chlordiazepoxide/amphetamine-induced hyperactivity mice model in vivo at 150 mg/kg.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₁H₁₈N₄O
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (50 mg/ml; light yellow solution)
      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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesChen, W., et al. 2011. ChemMedChem 6, 1587.