Cytosporone B

Cytosporone B (Csn-B;Dothiorelone G) is a naturally occurring nuclear orphan receptor Nur77 agonist with an EC50 of 0.278 nM.

Signaling Pathways >> Others >> Others

Research Areas >> Cancer

EC50: 0.278 nM (Nur77)[1]

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 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].

Human gastric cancer BGC-823 cells and human colon cancer SW620 cells are treated with cytosporone B for 72 h at 0-15 μg/mL. Cell viability is measured using the MTT assay[1].

Mice: The inoculated mice are randomly separated into two groups. One group is given an injection to the abdominal cavity at a dosage of 13 mg/kg of cytosporone B twice a week. The other group is administered with DMSO without cytosporone B. Food consumption and body weight of nude mice are monitored weekly. Four weeks later, the nude mice are killed and the tumors formed are removed, fixed and embedded[1].

[1]. Zhan Y, et al. Cytosporone B is an agonist for nuclear orphan receptor Nur77. Nat Chem Biol. 2008 Sep;4(9):548-56.

Captisol | Cyclosporin A | H2DCFDA | 0MPTP hydrochloride | GW4869 | Etomoxir | TD139 | Mitoquinone mesylate | GSK2795039 | JC-1 | BAPTA-AM | AP 20187 | Setanaxib (GKT137831) | D-Luciferin | Crotaline