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Axon 2337
CAS [725247-18-7]
MF C23H13F9N4O3SMW 596.42
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.
3-(4-(2,4-bis(trifluoromethyl)benzyloxy)-3-methoxyphenyl)-2-cyano-N-(5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl)acrylamide
[725247-18-7]
The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.
Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!
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