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361566 GSK-3 Inhibitor IV, SB-216763 - CAS 280744-09-4 - Calbiochem

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: SB-216763

361566
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
280744-09-4C₁₉H₁₂Cl₂N₂O₂

Products

Catalogue NumberPackaging Qty/Pack
361566-10MGCN Glass bottle 10 mg
Description
OverviewA cell-permeable (aryl,indole) maleimide compound that acts as a potent, selective, ATP-competitive inhibitor of GSK-3 activity (Ki = 9.1 nM for GSK-3α). At 10 µM concentration, does not significantly inhibit a panel of 24 other protein kinases tested. Reported to stimulate glycogen synthesis in Chang human liver cells (EC50 = 3.6 µM) and induce transcription of β-catenin-LEF/TCF (lymphoid enhancer factor/T cell factor) regulated reporter gene in HEK293 human embryonic kidney cell lines. Offers protection against polyglutamine-induced death in SK-N-SH and COS-7 cells and attenuates hypoxia-induced apoptosis in VSMC and COS-7 cells. Shown to reduce phosphoenolpyruvate carboxykinase (PEPCK) and glucose-6-phosphatase (G6Pase) expression in hepatoma cells. Promotes the survival of CLL lymphocytes via Wnt/β-catenin-mediated transcription activation. Exhibits delayed cardioprotection in vivo in a rat model via a KATP (ATP-sensitive potassium channels) and MPTP (mitochondrial permeability transition pore)-dependent mechanism at reperfusion.
Catalogue Number361566
Brand Family Calbiochem®
SynonymsSB-216763
References
ReferencesGross, E., et al. 2008. Am. J. Phy. Heart Circ Physiol. 294, H1497.
Bain, J., et al. 2007. Biochem. J. 408, 297.
Lu, D., et al. 2004. PNAS. 101, 3118.
Carmichael, J., et al. 2002. J. Biol. Chem. 277, 33791.
Culbert, A.A., et al. 2001. FEBS Lett. 507, 288.
Lochhead, P.A., et al. 2001. Diabetes 50, 937.
Cross, D.A., et al. 2001. J. Neurochem. 77, 94.
Coghlan, M.P., et al. 2000. Chem. Biol. 7, 793.
Product Information
CAS number280744-09-4
FormOrange solid
Hill FormulaC₁₉H₁₂Cl₂N₂O₂
Chemical formulaC₁₉H₁₂Cl₂N₂O₂
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Purity≥98% by HPLC
Physicochemical Information
Dimensions
Materials Information
Toxicological Information
Safety Information according to GHS
Safety Information
R PhraseR: 36/37/38

Irritating to eyes, respiratory system 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 Ambient Temperature Only
Toxicity Irritant
Storage +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.
Packaging Information
Transport Information
Supplemental Information
Specifications
Global Trade Item Number
Catalogue Number GTIN
361566-10MGCN 04055977214246

Documentation

GSK-3 Inhibitor IV, SB-216763 - CAS 280744-09-4 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

GSK-3 Inhibitor IV, SB-216763 - CAS 280744-09-4 - Calbiochem Certificates of Analysis

TitleLot Number
361566

References

Reference overview
Gross, E., et al. 2008. Am. J. Phy. Heart Circ Physiol. 294, H1497.
Bain, J., et al. 2007. Biochem. J. 408, 297.
Lu, D., et al. 2004. PNAS. 101, 3118.
Carmichael, J., et al. 2002. J. Biol. Chem. 277, 33791.
Culbert, A.A., et al. 2001. FEBS Lett. 507, 288.
Lochhead, P.A., et al. 2001. Diabetes 50, 937.
Cross, D.A., et al. 2001. J. Neurochem. 77, 94.
Coghlan, M.P., et al. 2000. Chem. Biol. 7, 793.
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.

Revision14-August-2012 JSW
SynonymsSB-216763
DescriptionA cell-permeable (aryl,indole) maleimide compound that acts as a potent, selective, ATP-competitive inhibitor of GSK-3 activity (Ki = 9.1 nM for GSK-3α). At 10 µM concentration, does not significantly inhibit a panel of 24 other protein kinases tested. Reported to stimulate glycogen synthesis in Chang human liver cells (EC50 = 3.6 µM) and induce transcription of β-catenin-LEF/TCF (lymphoid enhancer factor/T cell factor) regulated reporter gene in HEK293 human embryonic kidney cell lines. Offers protection against polyglutamine-induced death in SK-N-SH and COS-7 cells and attenuates hypoxia-induced apoptosis in VSMC and COS-7 cells. Shown to reduce phosphoenolpyruvate carboxykinase (PEPCK) and glucose-6-phosphatase (G6Pase) expression in hepatoma cells. Promotes the survival of CLL lymphocytes via Wnt/β-catenin-mediated transcription activation. Exhibits delayed cardioprotection in vivo in a rat model via a KATP (ATP-sensitive potassium channels) and MPTP (mitochondrial permeability transition pore)-dependent mechanism at reperfusion.
FormOrange solid
CAS number280744-09-4
Chemical formulaC₁₉H₁₂Cl₂N₂O₂
Structure formulaStructure formula
Purity≥98% by HPLC
SolubilityDMSO (50 mg/ml)
Storage +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 Irritant
ReferencesGross, E., et al. 2008. Am. J. Phy. Heart Circ Physiol. 294, H1497.
Bain, J., et al. 2007. Biochem. J. 408, 297.
Lu, D., et al. 2004. PNAS. 101, 3118.
Carmichael, J., et al. 2002. J. Biol. Chem. 277, 33791.
Culbert, A.A., et al. 2001. FEBS Lett. 507, 288.
Lochhead, P.A., et al. 2001. Diabetes 50, 937.
Cross, D.A., et al. 2001. J. Neurochem. 77, 94.
Coghlan, M.P., et al. 2000. Chem. Biol. 7, 793.