z-guggulsterone

z-guggulsterone is a plant-derived sterol found in the gum resin of the *Commiphora mukul* tree, traditionally used in Ayurvedic medicine. It acts as a potent antagonist of the Farnesoid X Receptor (FXR), a nuclear receptor involved in bile acid metabolism and immune regulation. Recent research, including studies presented at AACR 2025, highlights its potential in oncology for inhibiting FXR signaling in tumor-associated myeloid cells, such as myeloid-derived suppressor cells (MDSCs) and M2 macrophages. By blocking FXR, z-guggulsterone reduces the immunosuppressive activity of these cells, enhances antigen presentation, and promotes anti-tumor T-cell infiltration, thereby delaying tumor progression and improving the efficacy of adoptive T-cell therapies in models like melanoma.

Other names

(Z)-guggulsterone(Z)-4,17(20)-pregnadiene-3,16-dione