The liver X receptors (LXRs) are nuclear receptors that act as ligand-dependent transcription factors. They modulate lipid, cholesterol, and carbohydrate metabolism and homeostasis. SR9243 is a cell-permeable LXR inverse agonist that induces LXR-corepressor interaction at nanomolar concentrations. It reduces cancer cell viability (IC50 values range from 15 to 104 nM) without cytotoxicity against non-malignant cells. SR9243 disrupts the Warburg effect in cancer cells, suppressing the expression of glycolytic and lipogenic genes and reducing glycolytic metabolites and lipid production. It is effective in vivo, blocking glycolytic and lipogenic gene expression and inducing apoptosis in colon cancer xenografts without inducing weight loss in mice.
