Cytosporone B

Cytosporone B (Csn-B; Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77/NR4A1 agonist with an EC₅₀ of 0.278 nM. IC50 & Target:EC50: 0.278 nM (Nur77)^[1] In Vitro: Cytosporone B targets the ligand binding domain of Nur77, which selectively stimulates the transactivational activity of Nur77. Cytosporone B induces luciferase activity in cells that are cotransfected with GAL4- Nur77 or GAL4-LBD. The EC₅₀ of cytosporone B for Nur77 is 0.278 nM. Cytosporone B displays robust pro-apoptotic activity in gastric cancer cells BGC-823. 63.5% of the cells are apoptotic when treated with cytosporone B for 48 h. Cytosporone B shows selective effect on cancerous cells. Cytosporone B inhibits proliferation of human gastric cancer BGC-823 cells and human colon cancer SW620 cells by 470%, but it has a modest effect on human lung cancer H1299 cells and human hepatoma HepG2 cells^[1]. In Vivo: In the hepatocytes of wild-type mice, the transcriptional activity of the reporter is induced five-fold with cytosporone B treatment. In wild-type mice, cytosporone B treatment significantly increases glucose levels from 3.2 to 11.4 mM within the first 30 min, and thereafter blood glucose gradually decreased before reaching the initial level after 300 min^[1].