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

Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
487021-52-3C₁₂H₁₂N₄O₄S

Products

Catalogue NumberPackaging Qty/Pack
361549-5MG Plastic ampoule 5 mg
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
Global Trade Item Number
Catalogue Number GTIN
361549-5MG 04055977214055

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 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 Carcinogenic / Teratogenic
ReferencesNoble, W., et al. 2005. Proc. Natl. Acad. Sci. USA 102, 6990.
Bhat, R., et al. 2003. J. Biol. Chem. 278, 45937.