ERRα Antagonist

XCT-790 is a potent and selective inverse agonist for ERRα with an IC₅₀ value of 0.37 μM. XCT-790 induces cell death in chemotherapeutic resistant cancer cells. XCT-790 (Compound 12) is inactive against ERRγ and the estrogen receptors ERα and ERβ.

ERRα antagonist-1 (Compound A) is a selective and high affinity agonist for estrogen-related receptor α (ERRα). ERRα antagonist-1 inhibits interaction of ERRα with Proliferator-activated Receptor γ Coactivator-1α (PGC-1α) and PGC-1β, the IC₅₀ values are 170 nM and 180 nM, respectively.

PROTAC ERRα ligand 1 is a PROTAC target protein ligand. PROTAC ERRα ligand 1 is an orally active ERRα inverse agonist with IC₅₀ values of 0.6 μM for ERRα. PROTAC ERRα ligand 1 shows no significant activity against a panel of other nuclear receptors, including ERα^c, ERRγ, ERβ, PPARα, PPARγ, PPARδ, and RXRα. PROTAC ERRα ligand 1 can provide enhanced insulin sensitivity in vivo. PROTAC ERRα ligand 1 can be used for metabolic diseases research, such as type 2 diabetes and obesity.

ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC₅₀ of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo.