XCT790 is an inverse agonist of estrogen-related receptor α (ERRα; IC50 = ~300-500 nM). It demonstrates 90-100% inhibition of ERRα constitutive activity and has no significant activity at related nuclear receptors at 10 μM. XCT790 associates with the ligand-binding domain of ERRα and blocks ERRα/PGC-1α-dependent signaling, suppressing the expression of monoamine oxidases A and B. XCT790 induces proteasomal degradation of ERRα and potentiates the degradation of the estrogen receptor ERα by fulvestrant .
용도
XCT790 is a potent inverse agonist of ERRα.
Biochem/physiol Actions
XCT 790 is a 5′adenosine monophosphate-activated protein kinase (AMPK) activator. It also acts as a proton ionophore and an uncoupler of oxidative phosphorylation in mitochondria. XCT790 impairs vascular endothelial growth factor (VEGF) and angiopoietin 2 (Ang-2) expression and exhibits suppression of endometrial tumor via estrogen-related receptor (ERRα) inhibition. XCT790 mediates cell cycle arrest and favors apoptosis in triple-negative breast cancer (TNBC).
