CHIR99021 has been found to have both clinical and experimental utility; it induces insulin-responsive glucose uptake in insulin-resistant murine hepatocytes, and thus has extensive implications in the induction of hypoglycemia and the acute treatment of symptoms of the diabetic pathological phenotype. It has been previously demonstrated that other GSK3β inhibitors, specifically BIO-Acetoxime, activate the Wnt signaling pathway in human and murine embryonic stem (ES) cells, and CHIR99021 has indeed been shown to allow for long-term expansion of murine embryonic stem cells in a chemically-defined medium in conjunction with MEK/MAPK inhibitor PD184352 and fibroblast growth factor receptor (FGFR) inhibitor SU5402.
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