AS-1842856 is a potent inhibitor of forkhead box class O transcription factor 1 (Foxo1) with IC50 of 33 nM in HepG2 cells which directly bind to the active Foxo1.
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The forkhead box protein O1 (Foxo1) is a transcription factor that plays a critical role in hepatic gluconeogenesis. AS-1842856 is a Foxo1 inhibitor with an IC50 value of 0.03μM. In HepG2 cells transiently transfected with vectors carrying human Foxo1, AS-1842856 inhibited Foxo1 activity in a dose-dependent manner. AS-1842856 at a concentration of 0.1μM decreased Foxo1-mediated transactivation by 70%. Treatment of Fao cells with AS-1842856 for 18 hours inhibited the mRNA expression of G6Pase and PEPCK with IC50 values of 0.13μM and 0.037μM, respectively. Treatment of Fao cells with AS-1842856 (0.1 – 10μM) alone or in combination with insulin (0.1 – 10nM) did not affect the phosphorylation state of Akt, ERK, or S6K. In ICR mice, oral administration of AS-1842856 (100mg/kg) at three time points (8AM, 6PM, and 8AM on the second day) during 26-h fasting significantly reduced the mRNA expression of G6Pase and PEPCK in the liver, but did not alter the plasma glucose level.[3]
作用机制
AS-1842856 inhibits Foxo1-mediated transactivation by directly binding to Foxo1.[3]
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