Chemical Information

Biological Activity of XCT790

XCT-790 is a potent, selective and inverse agonist of estrogen-related receptor alpha(ERRα); induces cell death in chemotherapeutic resistant cancer cells.
IC50 value:
Target: ERRα
ERRalpha inverse agonist XCT-790 induced cell death in HepG2 hepatocarcinoma and its multi-drug resistance (MDR) sub-line R-HepG2. Using a dye Mitotracker Green which stains mitochondrion independent of mitochondrial membrane potential (DeltaPsi(m)), XCT-790 dose-dependently decreased mitochondrial mass. Intriguingly, XCT-790 increased DeltaPsi(m) upon short term treatment but decreased DeltaPsi(m) upon longer term treatment. XCT-790 synergized with paclitaxel to induce cell death in multi-drug resistance sub-line R-HepG2 [1].
XCT790 is a potent and specific inverse agonist of ERRα. XCT790 shows no significant antagonist activity on related nuclear receptors, such as ERR or ERα at concentrations below 10 μM. This also inhibits the constitutive activity of ER (Estrogen Receptor) [2].

References on XCT790

[1]. Wu F, et al. Estrogen-related receptor alpha (ERRalpha) inverse agonist XCT-790 induces cell death in chemotherapeutic resistant cancer cells. Chem Biol Interact. 2009 Oct 7;181(2):236-42.
[2]. Busch BB, et al. Identification of a selective inverse agonist for the orphan nuclear receptor estrogen-related receptor alpha. J Med Chem. 2004 Nov 4;47(23):5593-6.