XCT790

A potent and selective ERRα inverse agonist with IC50 of 300-500 nM in transient transfection assays; shows no significant antagonist activity on related nuclear receptors (ERRγ or ERα, LXRα, LXRβ, FXR, PPARα, PPARδ, PPARγ, Nurr1, RARα, RORα, and RXRα) at 10 uM; inhibits PGC-1α regulation of ERRα and ERRα target gene expression; inhibits proliferation in cellular models of breast cancer. (In Vitro) :XCT-790 (0-40 μM; 48 hours and 72 hours) reduces the viability of MES-SA, MES-SA/DX5, and HepG2 cells in a dose-dependent manner.XCT-790 (10 μM; 24 hours and 48 hours) reduces the protein levels of ERRα in HepG2 and R-HepG2 cell lines after 24 hours and maintains these reduced levels after 48 hours.XCT-790 (10 μM; 48 hours) induces apoptosis in the two cell lines with HepG2 being more sensitive compared to R-HepG2. (In Vivo) :XCT-790 (XCT790; 4 mg/kg; intravenous injection; every three days; for 3 weeks; BALB/c mice) significantly inhibits tumor growth and angiogenesis, and induces apoptosis without a reduction in body weight, in xenograft models.