CHIR-99021

A potent, specific GSK-3 inhibitor with IC50 of 5 nM and 10 nM for GSK3β and GSK3α, respectively; mimics Wnt signaling in preadipocytes, stabilizes free cytosolic beta-catenin and inhibits adipogenesis by blocking induction of C/EBPα and PPARγ; potentiates insulin activation of glucose transport and utilization in vitro and in vivo; also widely used for stem cell differentiation and naive stem cell generation. (In Vitro) :Laduviglusib (1-10 μM, 3 days) reduces the viability of the ES-D3 cells with an IC50 of 4.9 μM.Laduviglusib (5 μM, 48 h) activates the canonical Wnt-pathway in ES-D3 cells and ES-CCE cells.Laduviglusib (3 μM, 4 days) inhibits ES cell differentiation into neural cells.Laduviglusib (1 μM, 2 weeks) inhibits adipogenesis by blocking induction of C/EBPα and PPARγ in 3T3-L1 preadipocytes.Laduviglusib (2.5 μM, 24 h) protects Lgr5+ cells against radiation-induced apoptosis. (In Vivo) :Laduviglusib (30 mg/kg, p.o) rapidly lowers plasma glucose.Laduviglusib (2 mg/kg, i.p.) protects mice against radiation-induced lethal GI injury.