AS1842856 is a Foxo1 inhibitor (IC50=30 nM) that specifically blocks the transcriptional activity of Foxo1 and reduces its activity by directly binding to activated FoxO1. AS1842856 has autophagy inhibitory activity.

FOXO1:33nM

METHODS: Human monocytes were treated with BAY 2416964 (1 nM-10 µM), kynurenic acid (200 µM), and LPS (10 ng/mL) for 24 h. TNF-α levels were measured by ELISA.
RESULTS: kynurenic acid-induced AhR activation inhibited TNF-α production in LPS-stimulated monocytes, and BAY 2416964 dose-dependently rescued this AhR-mediated inhibition. [1]

METHODS: To assay antitumor activity in vivo, BAY 2416964 (30 mg/kg) was administered orally to NSG mice bearing B16F10-OVA tumors once daily for seven days.
RESULTS: BAY 2416964 inhibited tumor growth.BAY 2416964 increased the frequency of immunostimulatory tumor-infiltrating CD8+ T cells and N cells, and decreased the frequency of immunosuppressive GR1-positive myeloid cells and CD206+M2 macrophages. [1]

Fao cells are serum-starved (1 h) and incubated for 30 min with either insulin or AS1842856 at the indicated concentration. Protein lysates are prepared from cells treated with either insulin or AS1842856, and relative concentration of phosphorylated Foxo1 protein is determined by Western blot analysis. (Only for Reference)