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361549 GSK-3β Inhibitor VIII - CAS 487021-52-3 - Calbiochem

Overview

Replacement Information

Key Specifications Table

Empirical Formula
C₁₂H₁₂N₄O₄S

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361549-5MG
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      Description
      OverviewA cell-permeable thiazole-containing urea compound that acts as a potent inhibitor of GSK-3. Shown to inhibit GSK-3β with high potency (IC50 = 104 nM). Inhibition is competitive with respect to ATP (Ki = 38 nM). Specificity has been reported using a panel of 28 different kinases, including Cdk2 and Cdk5 (IC50 > 100 µM). Shown to prevent tau phosphorylation at a GSK-3-specific site. Also shown to protect neuronal cells against Aβ-mediated neurodegeneration in vitro and reduce tauopathy in mice in vivo (30 µmol/kg delivered with 40% PEG400 and 40% dimethylacetamide in water). Caution: Do not use delivering vehicles containing dimethylamine for in vivo studies, as it is highly toxic to animals. A 25 mM (5 mg/649 µl) solution of GSK-3β Inhibitor VIII (Cat. No. 361557) in DMSO is also available.
      Catalogue Number361549
      Brand Family Calbiochem®
      SynonymsAR-A014418, N-(4-Methoxybenzyl)-Nʹ-(5-nitro-1,3-thiazol-2-yl)urea
      References
      ReferencesNoble, W., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 6990.
      Bhat, R., et al. 2003. J. Biol. Chem. 278, 45937.
      Product Information
      CAS number487021-52-3
      ATP CompetitiveY
      FormYellow solid
      Hill FormulaC₁₂H₁₂N₄O₄S
      Chemical formulaC₁₂H₁₂N₄O₄S
      ReversibleN
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      ApplicationGSK-3β Inhibitor VIII, CAS 487021-52-3, is a cell-permeable, potent inhibitor of GSK-3 (IC50 = 104 nM). Inhibition is competitive with respect to ATP (Ki = 38 nM).
      Biological Information
      Primary TargetGsk-3β
      Primary Target IC<sub>50</sub>104 nM against GSK-3β
      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 Carcinogenic / Teratogenic
      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

      Documentation

      GSK-3β Inhibitor VIII - CAS 487021-52-3 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      GSK-3β Inhibitor VIII - CAS 487021-52-3 - Calbiochem Certificates of Analysis

      TitleLot Number
      361549

      References

      Reference overview
      Noble, W., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 6990.
      Bhat, R., et al. 2003. J. Biol. Chem. 278, 45937.
      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.

      Revision05-October-2007 JSW
      SynonymsAR-A014418, N-(4-Methoxybenzyl)-Nʹ-(5-nitro-1,3-thiazol-2-yl)urea
      DescriptionA cell-permeable, potent inhibitor of glycogen synthase kinase-3 (GSK-3). Shown to inhibit GSK-3β with high potency (IC50 = 104 nM). Inhibition is competitive with respect to ATP (Ki = 38 nM). Specificity has been reported using a panel of 28 different kinases, including Cdk2 and Cdk5 (IC50 >100 µM). Shown to prevent tau phosphorylation at a GSK-3-specific site. Also shown to protect neuronal cells against Aβ-mediated neurodegeneration in vitro and reduce tauopathy in mice in vivo (30 µmol/kg delivered with 40% PEG400 and 40% dimethylacetamide in water). Caution: Do not use delivering vehicles containing dimethylamine for in vivo studies, as it is highly toxic to animals.
      FormYellow solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number487021-52-3
      Chemical formulaC₁₂H₁₂N₄O₄S
      Structure formulaStructure formula
      Purity≥95% by HPLC
      SolubilityDMSO (5 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 3 months at -20°C.
      Toxicity Carcinogenic / Teratogenic
      ReferencesNoble, W., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 6990.
      Bhat, R., et al. 2003. J. Biol. Chem. 278, 45937.