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Potent and selective GSK3 inhibitor (Ki= 9 nM for GSK-3α). Has little activity against 24 other protein kinases (IC50 > 10 μM). Stimulates glycogen synthesis, gene transcription and is cardio- and neuroprotective.
SB 216763 is a potent and selective, ATP-competitive glycogen synthase kinase-3 (GSK-3) inhibitor. Equally effective at inhibiting human GSK-3α and GSK-3β. Exhibits minimal activity against 24 other protein kinases (IC50 >10 μM). 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.
SB 216763 maintains mouse embryonic stem (ES) cells in an undifferentiated, pluripotent state for up to two months when co-cultured with mouse embryonic fibroblasts (MEFs) in the absence of leukemia inhibitory factor (LIF; Kirby et al.) and increases neural progenitor proliferation in mouse brains (Mao et al.). SB 216763 has been found to induce differentiation and reduce the cancer stem cell population of cultured human glioblastoma cells (Korur et al.).
Alternative names: GSK-3 Inhibitor IV, SB-216763, SB-216763 Applications: Differentiation, Expansion, Maintenance Cell types: Cancer Cells and Cell Lines, Dendritic Cells, Hematopoietic Stem and Progenitor Cells, Mesenchymal Stem and Progenitor Cells, Myogenic Stem and Progenitor Cells, Neural Stem and Progenitor Cells, Pluripotent Stem Cells
Keywords: SB-216763, potent GSK-3, inhibitors, inhibits, kinases, carbohydrate, Metabolism, SB216763, Kinase, stem cell proliferation
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