In vitro activity: AS1842856 potently inhibits human Foxo1 transactivation and reduces glucose production through the inhibition of glucose-6 phosphatase and phosphoenolpyruvate carboxykinase mRNA levels in a rat hepatic cell line

Kinase Assay: AS1842856 is a potent and cell-permeable Foxo1 inhibitor with an IC50 of 30 nM.

Cell Assay: Rat hepatoma Fao cells are cultured in DMEM with 5.5 mM glucose and 10% FBS. Glucose production rate is measured using glucose CII-test reagent. In brief, after 18 h of treatment with either insulin or AS1842856 at the indicated concentrations, the cells are ished three times with PBS. The cells are then incubated for 3 h at 37°C in 5% CO2 in a glucose production buffer (glucose-free DMEM, pH 7.4, containing 20 mM sodium pyruvate, without phenol red).