| 產(chǎn)品名稱 | XCT 790 |
| 產(chǎn)品貨號 | Axon 2337 CAS [725247-18-7] MF C23H13F9N4O3SMW 596.42 Purity: 99% Soluble in DMSO 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. References Certificates Categories Extra info 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. Certificate of Analysis Material Safety Data Sheet Apoptosis Cell Signaling & Oncology Diabetes & Metabolism Endocrinology Unclassified ERRα NR3B ERRα inverse agonist and potent mitochondrial uncoupler Chemical name 3-(4-(2,4-bis(trifluoromethyl)benzyloxy)-3-methoxyphenyl)-2-cyano-N-(5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl)acrylamide Parent CAS No. [725247-18-7] Order Size Unit Price Stock 10 mg €120.00 In Stock |
| 產(chǎn)品價(jià)格 | 現(xiàn)貨詢價(jià)，電話：010-67529703 |
| 產(chǎn)品規(guī)格 | |
| 產(chǎn)品品牌 | axonmedchem |
| 產(chǎn)品概述 | |
| 產(chǎn)品詳情 |
XCT 790Axon 2337 CAS [725247-18-7] MF C23H13F9N4O3S
DescriptionEstrogen-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.
ERRα inverse agonist and potent mitochondrial uncoupler
Chemical name3-(4-(2,4-bis(trifluoromethyl)benzyloxy)-3-methoxyphenyl)-2-cyano-N-(5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl)acrylamide Parent CAS No.[725247-18-7] |
| 產(chǎn)品資料 |
