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XCT 790
- Soluble in DMSO
- MF: C23H13F9N4O3S
- MW: 596.42
Description
Estrogen-related receptor α (ERRα) inverse agonist (IC50 value of ~300–500 nM) and potent mitochondrial uncoupler that induces cell death in chemotherapeutic resistant cancer cells by causing mitochondrial dysfunction. XCT790 was found to potently activate AMPK in a dose-dependent and ERRα-independent manner at concentrations more than 25-fold below those typically used to perturb ERRα. Measurements of mitochondrial membrane potential, oxygen consumption, and extracellular acidification rates indicated acute and dose-dependent uncoupling of oxidation from phosphorylation in mitochondria by XCT 790. It modulates the activity of ERRα and reduces the proliferation of various cell lines by blocking the G1/S transition of the cell cycle in an ERRα-dependent manner. XCT 790 showed no activity towards a wide range of (GAL4-chimeric) receptors.
More Information
| Parent CAS No. | 725247-18-7 |
|---|---|
| Chemical Name | 3-(4-(2,4-bis(trifluoromethyl)benzyloxy)-3-methoxyphenyl)-2-cyano-N-(5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl)acrylamide |
| SMILES | C(NC1=NN=C(C(F)(F)F)S1)(=O)/C(/C#N)=C/C1=CC=C(OCC2=CC=C(C(F)(F)F)C=C2C(F)(F)F)C(OC)=C1 |
| MFCD | MFCD08277031 |
| InChi | InChI=1S/C23H13F9N4O3S/c1-38-17-7-11(6-13(9-33)18(37)34-20-36-35-19(40-20)23(30,31)32)2-5-16(17)39-10-12-3-4-14(21(24,25)26)8-15(12)22(27,28)29/h2-8H,10H2,1H3,(H,34,36,37)/b13-6+ |
| InChiKey | HQFNFOOGGLSBBT-AWNIVKPZSA-N |
| CID | 6918788 |
| Short Description | ERRα inverse agonist/Apoptosis inducer |
References
- B. Eskiocak et al. The estrogen-related receptor α inverse agonist XCT 790 is a nanomolar mitochondrial uncoupler. Biochemistry. 2014 Jul 29;53(29):4839-46.
- F. Wu 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.
- S. Bianco et al. Modulating estrogen receptor-related receptor-alpha activity inhibits cell proliferation. J Biol Chem. 2009 Aug 28;284(35):23286-92.
- O. Lanvin et al. Potentiation of ICI182,780 (Fulvestrant)-induced estrogen receptor-alpha degradation by the estrogen receptor-related receptor-alpha inverse agonist XCT790. J Biol Chem. 2007 Sep 28;282(39):28328-34.
- P.J. Willy et al. Regulation of PPARgamma coactivator 1alpha (PGC-1alpha) signaling by an estrogen-related receptor alpha (ERRalpha) ligand. Proc Natl Acad Sci U S A. 2004 Jun 15;101(24):8912-7.
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