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361571 InSolution™ GSK-3 Inhibitor XVI, CHIR99021 - CAS 252917-06-9 - Calbiochem

361571
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Overview

Replacement Information

Key Spec Table

Empirical FormulaCAS #
C₂₂H₁₈Cl₂N₈252917-06-9

Products

Catalogue NumberPackaging Qty/Pack
361571-5MG Glass bottle 5 mg
Description
OverviewA 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 Number361571
Brand Family Calbiochem®
Synonyms6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile
References
ReferencesMussmann, 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.
Product Information
CAS number252917-06-9
FormLiquid
FormulationA 25 mM (5 mg/430 µL) solution of GSK-3 Inhibitor XVI, CHIR99021 (Cat. No. 361559) in DMSO.
Hill FormulaC₂₂H₁₈Cl₂N₈
Hygroscopic Hygroscopic
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetGSK-3 α and β
Primary Target IC<sub>50</sub>10 and 6.7 nM against GSK-3&alpha
Purity≥95% by HPLC
Physicochemical Information
Cell permeableY
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
R PhraseR: 36/38

Irritating to eyes and skin.
S PhraseS: 26-36

In case of contact with eyes, rinse immediately with plenty of water and seek medical advice.
Wear suitable protective clothing.
Product Usage Statements
Storage and Shipping Information
Ship Code Dry Ice Only
Toxicity Irritant
Storage ≤ -70°C
Protect from Light Protect from light
Hygroscopic Hygroscopic
Avoid freeze/thaw Avoid freeze/thaw
Do not freeze Ok to freeze
Special InstructionsFollowing initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.
Packaging Information
Packaged under inert gas Packaged under inert gas
Transport Information
Supplemental Information
Specifications

Documentation

InSolution™ GSK-3 Inhibitor XVI, CHIR99021 - CAS 252917-06-9 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

InSolution™ GSK-3 Inhibitor XVI, CHIR99021 - CAS 252917-06-9 - Calbiochem Certificates of Analysis

TitleLot Number
361571

References

Reference overview
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

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.

Revision21-September-2012 JSW
Synonyms6-(2-(4-(2,4-Dichlorophenyl)-5-(4-methyl-1H-imidazol-2-yl)-pyrimidin-2-ylamino)ethyl-amino)-nicotinonitrile
DescriptionA 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.
FormLiquid
FormulationA 25 mM (5 mg/430 µL) solution of GSK-3 Inhibitor XVI, CHIR99021 (Cat. No. 361559) in DMSO.
Intert gas (Yes/No) Packaged under inert gas
CAS number252917-06-9
Structure formulaStructure formula
Purity≥95% by HPLC
Storage ≤ -70°C
Hygroscopic
Protect from light
Avoid freeze/thaw
Do Not Freeze Ok to freeze
Special InstructionsFollowing initial thaw, aliquot and freeze (-70°C). Aliquots are stable for up to 6 months at -70°C.
Toxicity Irritant
ReferencesMussmann, 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.