Retinoic acid receptor-related orphan receptors α and γ (RORα and RORγ) have been demonstrated to play important roles in the regulation of metabolism, circadian rhythms, immune function, and tumorigenesis. SR 1078 is a selective agonist of RORα and RORγ that stimulates ROR transcriptional activity in HEK293 cell reporter assays at concentrations as low as 2 μM without effect at the related liver X receptors and farnesoid X receptors. At 5 μM, SR 1078 has been shown to stabilize p53 and to induce apoptosis in HepG2 cancer cells.
