SB216763

SB216763 is a cell-permeable ATP-competitive inhibitor of glycogen synthase kinase 3α (GSK3α, IC₅₀ = 34 nM) and GSK3β isozymes (Coghlan et al.). GSK3 is a serine/threonine protein kinase that is inhibited by a variety of extracellular stimuli including insulin, growth factors, cell specification factors, and cell adhesion.

MAINTENANCE AND SELF-RENEWAL

• 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.).
• Promotes the proliferation of primary mouse retinal stem cells (Inoue et al.).
• Increases neural progenitor proliferation in mouse brains (Mao et al.).
• Increases symmetric division of neural stem cells (NSCs) in in vivo and in vitro models of the adult mouse brain (Piccin and Morshead).
• Inhibits adipocyte differentiation in human mesenchymal stem cells (MSCs; Shen et al.).
• Promotes the generation of hematopoietic stem cells (HSCs) in aorta-gonad-mesonephros (AGM) explant cultures (Ruiz-Herguido et al.).

DIFFERENTIATION

• Enhances the insulin-induced differentiation of quiescent reserve cells from cultured mouse myoblasts (Rochat et al.).
• Stimulates NSC differentiation in cultured rat neurospheres (Maurer et al.).
• Induces neuronal differentiation in cultured human neural progenitor cells (NPCs; Lange et al.).
• Promotes differentiation of dendritic cells from cultured mouse hematopoietic progenitor cells (HPCs; Zhou et al.).

CANCER RESEARCH

• Induces differentiation and reduces the cancer stem cell population of cultured human glioblastoma cells (Korur et al.).