MilliporeSigma™ Calbiochem™ InSolution™ Foxo1 Inhibitor, AS1842856

Description

• A cell-permeable oxodihydroquinoline that preferentially inhibits the transcription activity of Forkhead box O family member Foxo1 over that of the functionally related Foxo3a and Foxo4 (70%, 20%, and 3% inhibition, respectively, in HepG2-based reporter assays; [AS184256] = 100nM) in a dose-dependent manner (IC 50 = 33nM) via direct binding of the non-Ser256-phosphorylated/active Foxo1, but not the Ser256-phosphorylated/inactive form of Foxo1
• Shown to inhibit gluconeogenesis in rat heptoma Fao cultures (IC 50 = 37 and 130nM against PEPCK and G6Pase mRNA level; IC 50 = 43nM against glucose production) in vitro and in murine liver of both normoglycemic ICR mice (60% and 45% inhibition of hepatic G6Pase and PEPCK mRNA level, respectively; three 100mg/kg p.o
• dosages at 0, 12, 24 h) and diabetic db/db mice (86%, 70%, 56%, 48%, 35%, and 31% inhibition of hepatic G6Pase, ABCG8, ABCG5, PEPCK, IL-1β, and apoCIII mRNA level, respectively; three 100mg/kg p.o
• dosages at 0, 12, 24 h) during a 26-hour fasting period in vivo .