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SB 216763

Chemical Structure : SB 216763

CAS No.: 280744-09-4

SB 216763 (SB-216763;SB216763)

Catalog No.: PC-42827Not For Human Use, Lab Use Only.

SB 216763 is a potent, selective, ATP competitive and cell permeable inhibitor GSK-3 with Ki of 9 nM (GSK-3α), equally potent for GSK-3β.

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Biological Activity

SB 216763 is a potent, selective, ATP competitive and cell permeable inhibitor GSK-3 with Ki of 9 nM (GSK-3α), equally potent for GSK-3β.
SB 216763 displays no significant activity against a panel of 24 other protein kinases.
SB 216763 stimulates glycogen synthesis in human liver cells and induces expression of a beta-catenin-LEF/TCF regulated reporter gene in HEK293 cells, protects both central and peripheral nervous system neurones in culture from death, activates beta-catenin-mediated transcription, and enhances the survival of CLL lymphocytes.
SB 216763 displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis.

Physicochemical Properties

M.Wt 371.2168
Formula C19H12Cl2N2O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1H-Pyrrole-2,5-dione, 3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-

References

1. Coghlan MP, et al. Chem Biol. 2000 Oct;7(10):793-803.

2. Cross DA, et al. J Neurochem. 2001 Apr;77(1):94-102.

3. Lu D, et al. Proc Natl Acad Sci U S A. 2004 Mar 2;101(9):3118-23.

4. Gurrieri C, et al. J Pharmacol Exp Ther. 2010 Mar;332(3):785-94.

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