361571 Sigma-AldrichInSolution™ GSK-3 Inhibitor XVI, CHIR99021 - CAS 252917-06-9 - Calbiochem
InSolution™ GSK-3 Inhibitor XVI, CHIR99021, CAS 252917-06-9, is a 25 mM solution in DMSO. A cell-permeable, ATP-competitive inhibitor of GSK-3 (IC₅₀ = 10 & 6.7 nM for GSK-3α and GSK-3β, respectively).
More>> InSolution™ GSK-3 Inhibitor XVI, CHIR99021, CAS 252917-06-9, is a 25 mM solution in DMSO. A cell-permeable, ATP-competitive inhibitor of GSK-3 (IC₅₀ = 10 & 6.7 nM for GSK-3α and GSK-3β, respectively). Less<<Synonyms: 6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile
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Overview
Replacement Information |
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Key Spec Table
CAS # | Empirical Formula |
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252917-06-9 | C₂₂H₁₈Cl₂N₈ |
Products
Catalogue Number | Packaging | Qty/Pack | |
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361571-5MGCN | Glass bottle | 5 mg |
Description | |
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Overview | A cell-permeable aminopyrimidine compound that acts as potent, ATP-competitive, and highly selective GSK-3 inhibitor (IC50 = 10 and 6.7 nM against GSK-3α and GSK-3β, respectively). Exhibits little or no activity toward 46 other enzymes (IC50 >8.8 µM against 20 kinases and Ki ≥5 µM against 23 non-kinase enzymes) and shows only weak binding to 22 pharmacologically relevant receptors (Kd ~4 µM). This compound is orally available and is shown to effectively improve glucose metabolism in both murine and rat type 2 diabetes models in vivo. The solid form of this compound (Cat. No. 361559) is also available. |
Catalogue Number | 361571 |
Brand Family | Calbiochem® |
Synonyms | 6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile |
Product Information | |
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CAS number | 252917-06-9 |
Form | Liquid |
Formulation | A 25 mM (5 mg/430 µL) solution of GSK-3 Inhibitor XVI, CHIR99021 (Cat. No. 361559) in DMSO. |
Hill Formula | C₂₂H₁₈Cl₂N₈ |
Hygroscopic | Hygroscopic |
Reversible | Y |
Structure formula Image | |
Quality Level | MQ100 |
Applications |
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Biological Information | |
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Primary Target | GSK-3 α and β |
Primary Target IC<sub>50</sub> | 10 and 6.7 nM against GSK-3&alpha |
Purity | ≥90% by HPLC |
Physicochemical Information | |
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Cell permeable | Y |
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Materials Information |
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Toxicological Information |
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Safety Information according to GHS |
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Product Usage Statements |
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Packaging Information | |
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Packaged under inert gas | Packaged under inert gas |
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Supplemental Information |
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Specifications |
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Global Trade Item Number | |
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Catalogue Number | GTIN |
361571-5MGCN | 04055977213577 |
Documentation
InSolution™ GSK-3 Inhibitor XVI, CHIR99021 - CAS 252917-06-9 - Calbiochem SDS
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InSolution™ GSK-3 Inhibitor XVI, CHIR99021 - CAS 252917-06-9 - Calbiochem Certificates of Analysis
Title | Lot Number |
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361571 |
References
Reference overview |
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Mussmann, R., et al. 2007. J. Biol. Chem. 282, 12030. Ring, D.B., et al. 2003. Diabetes 52, 588. Bennett, C.N., et al. 2002. J. Biol. Chem. 277, 30998. Cline, G.W., et al. 2002. Diabetes 51, 2903. |
Data Sheet | ||||||||||||||||||||||||||||
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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.
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