AS1842856

AS-1842856 is a potent inhibitor of forkhead box class O transcription factor 1 (FoxO1; IC₅₀ = 33 nM in HepG2 cells). Inhibition of FoxO1-mediated transactivation with AS-1842856 leads to a dose-dependent decrease in expression of glucose-6 phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK) mRNA and inhibits glucogenesis in rat hepatoma Fao cells and a murine model of type 2 diabetes mellitus (T2DM). AS-1842856 also inhibits 3T3-L1 preadipocyte differentiation and reduces lipid droplet growth in adipocytes.,

AS 1842856 is a novel FoxO1 antagonist with anti-obesity effects.

ChEBI: AS1842856 is a quinolone that is 4-quinolone substituted at positions 1, 3, 5, 6 and 7 by ethyl, carboxy, amino, fluorine, and cyclohexylamino groups, respectively. It can directly bind to and block the transcription activity of the active forkhead box protein O1 (Foxo1), but not the Ser256-phosphorylated form. It induces cell death and growth arrest in Burkitt lymphoma cell lines at low concentrations. It has a role as a hypoglycemic agent, an anti-obesity agent, an autophagy inhibitor, an antineoplastic agent, an apoptosis inducer and a forkhead box protein O1 inhibitor. It is a quinolinemonocarboxylic acid, a quinolone, an organofluorine compound, a primary amino compound, a secondary amino compound and a tertiary amino compound.

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[1] TAKEYUKI NAGASHIMA. Discovery of novel forkhead box O1 inhibitors for treating type 2 diabetes: improvement of fasting glycemia in diabetic db/db mice.[J]. ACS Applied Electronic Materials, 2010: 961-970. DOI: 10.1124/mol.110.065714
[2] LONGHUA LIU. FoxO1 antagonist suppresses autophagy and lipid droplet growth in adipocytes.[J]. Cell Cycle, 2016, 15 15: 2033-2041. DOI: 10.1080/15384101.2016.1192732
[3] PENG ZOU. Targeting FoxO1 with AS1842856 suppresses adipogenesis.[J]. Cell Cycle, 2014, 13 23: 3759-3767. DOI: 10.4161/15384101.2014.965977