CHIR-99021 (252917-06-9) is a potent and selective inhibitor of glycogen synthase kinase-3β (GSK3β, IC50 = 5 nM) and GSK3α (IC50 = 10 nM)1. Induces osteoblastogenesis, increases mineralization and inhibits adipogenesis in ST2 cells2. Promotes replication and survival of pancreatic beta cells3. CHIR-99021 enhances differentiation and reduces proliferation of adult human olfactory epithelium neural precursors4. Cell permeable and active in vivo.
References/ CHIR99021 Citations
1) Bennett et al. (2002), Regulation of Wnt signaling during adipogenesis; J. Biol. Chem., 277 30998
2) Bennett et al. (2005), Regulation of osteoblastogenesis and bone mass by Wnt10b; Proc. Natl. Acad. Sci. USA, 102 3324
3) Mussmann et al. (2007), Inhibition of GSK3 promotes replication and survival of pancreatic beta cells; J. Biol. Chem., 282 12030
4) Manceur et al. (2011), Inhibition of glycogen synthase kinase-3 enhances the differentiation and reduces the proliferation of adult human olfactory epithelium neural precursors; Exp. Cell. Res., 317 2086
5) Takaoka et al. (2016), Live imaging of transforming growth factor-β activated kinase 1 activation in Lewis Lung carcinoma 3LL cells implanted into syngeneic mice and treated with polyinosinic:polycytidylic acid; Cancer Sci., 107 644 [Focus Citation]