Potent and selective, ATP-competitive glycogen synthase kinase-3 (GSK-3) inhibitor (IC50
= 34.3 nM for GSK-3α
). Equally effective at inhibiting human GSK-3α
. Exhibits minimal activity against 24 other protein kinases (IC50
M). Stimulates glycogen synthesis in liver cells, and induces β
-catenin-dependent gene transcription. Neuroprotective; also reduces pulmonary inflammation and fibrosis in a mouse model. Shown to maintain mouse embryonic stem cells in a pluripotent state.
Soluble to 75 mM in DMSO
Store at RT
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All Tocris products are intended for laboratory research use only.
Sold for research purposes under agreement from GlaxoSmithKline
3-(2,4-dichlorophenyl)-4-(1-methyl-1H-indol-3-yl)-1H-pyrrole-2,5-dione (SB216763), a glycogen synthase kinase-3 inhibitor, displays therapeutic properties in a mouse model of pulmonary inflammation and fibrosis.
Gurrieri et al.
Regulation and function of glycogen synthase kinase-3 isoforms in neuronal survival.
Liang and Chuang
Selective small molecule inhibitors of glycogen synthase kinase-3 modulate glycogen metabolism and gene transcription.
Coghlan et al.
Selective small-molecule inhibitors of glycogen synthase kinase-3 activity protect primary neurones from death.
Cross et al.
Glycogen synthase kinase 3 (GSK3) inhibitor, SB-216763, promotes pluripotency in mouse embryonic stem cells.
Kirby et al.
PLoS One, 2012;7:e39329
The citations listed below are publications that use Tocris products. Selected citations for SB 216763 include:
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