AS1842856

AS1842856 is a potent, cell-permeable, and orally active small-molecule inhibitor of the Forkhead box O1 (FoxO1) transcription factor. Originally discovered by Astellas Pharma for the treatment of type 2 diabetes, AS1842856 directly binds to the active, unphosphorylated form of FoxO1, blocking its DNA-binding and transcriptional activity. This inhibition suppresses the expression of key gluconeogenic enzymes, such as glucose-6-phosphatase (G6Pase) and phosphoenolpyruvate carboxykinase (PEPCK), thereby reducing hepatic glucose production. Beyond its metabolic applications, AS1842856 has been widely utilized as a chemical probe in preclinical research to investigate FoxO1's role in oncology (such as leukemia, lymphoma, and glioblastoma), neurodegenerative diseases (where it has also been shown to directly inhibit GSK3 alpha/beta and promote its exocytosis), and acute-on-chronic liver failure.

Other names

5-amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-1,4-dihydro-4-oxo-3-quinolinecarboxylic acid5-amino-7-(cyclohexylamino)-1-ethyl-6-fluoro-4-oxo-1,4-dihydroquinoline-3-carboxylic acid