SR1078

SR1078 is a synthetic, cell-permeable small molecule agonist of the retinoic acid receptor-related orphan receptors alpha (RORα) and gamma (RORγ). Developed by researchers at The Scripps Research Institute, SR1078 directly binds to the ligand-binding domains of RORα and RORγ, inducing conformational changes that stimulate their transcriptional activity. This leads to the upregulation of ROR target genes, such as glucose-6-phosphatase (G6Pase) and fibroblast growth factor 21 (FGF21). In preclinical oncology models, SR1078 has been shown to stabilize the tumor suppressor protein p53, inducing cell-cycle arrest and apoptosis in cancer cells, including hepatocellular carcinoma. Additionally, SR1078 has been investigated for its potential to restore circadian clock function (by upregulating BMAL1) to attenuate MYC-driven oncogenesis and proliferation in lung cancer, as well as for reducing repetitive behaviors in animal models of autism spectrum disorder.

Other names

N-[4-[2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl]phenyl]-4-(trifluoromethyl)benzamide