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

361549
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₂H₁₂N₄O₄S 487021-52-3

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      361549-5MG
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          Plastic ampoule 5 mg
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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
          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

          SDS

          Title

          Safety Data Sheet (SDS) 

          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.