| Identification | Back Directory | [Name]
XCT 790 | [CAS]
725247-18-7 | [Synonyms]
CS-1881
XCT 790; XCT-790
3-[4-(2,4-bis-trifluoromethylbenzyloxy)-3-methoxyphenyl]-2-cyano-n-(5-trifluoromethyl-1,3,4-thiadiazol-2-yl)acrylamide
2-Propenamide, 3-[4-[[2,4-bis(trifluoromethyl)phenyl]methoxy]-3-methoxyphenyl]-2-cyano-N-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]-
(E)-3-[4-[[2,4-bis(trifluoromethyl)phenyl]methoxy]-3-methoxyphenyl]-2-cyano-N-[5-(trifluoromethyl)-1,3,4-thiadiazol-2-yl]prop-2-enamide
3-[4-[[2,4-Bis(trifluoromethyl)benzyl]oxy]-3-methoxyphenyl]-2-cyano-N-(5-trifluoromethyl-[1,3,4]thiadiazol-2-yl)acrylamide XCT 790
XCT 790 3-[4-[[2,4-Bis(trifluoromethyl)benzyl]oxy]-3-methoxyphenyl]-2-cyano-N-(5-trifluoromethyl-[1,3,4]thiadiazol-2-yl)acrylamide | [Molecular Formula]
C23H13F9N4O3S | [MDL Number]
MFCD08277031 | [MOL File]
725247-18-7.mol | [Molecular Weight]
596.42 |
| Hazard Information | Back Directory | [Description]
XCT790 is an inverse agonist of estrogen-related receptor α (ERRα; IC50 = ~300-500 nM). It demonstrates 90-100% inhibition of ERRα constitutive activity and has no significant activity at related nuclear receptors at 10 μM. XCT790 associates with the ligand-binding domain of ERRα and blocks ERRα/PGC-1α-dependent signaling, suppressing the expression of monoamine oxidases A and B. XCT790 induces proteasomal degradation of ERRα and potentiates the degradation of the estrogen receptor ERα by fulvestrant . | [Uses]
XCT790 is a potent inverse agonist of ERRα. | [Definition]
ChEBI: XCT 790 is a member of cinnamamides. | [Biochem/physiol Actions]
XCT 790 is a 5′adenosine monophosphate-activated protein kinase (AMPK) activator. It also acts as a proton ionophore and an uncoupler of oxidative phosphorylation in mitochondria. XCT790 impairs vascular endothelial growth factor (VEGF) and angiopoietin 2 (Ang-2) expression and exhibits suppression of endometrial tumor via estrogen-related receptor (ERRα) inhibition. XCT790 mediates cell cycle arrest and favors apoptosis in triple-negative breast cancer (TNBC). | [storage]
Store at +4°C | [References]
[1] lu x, peng l, lv m, ding k. recent advance in the design of small molecular modulators of estrogen-related receptors. curr pharm des. 2012;18(23):3421-31.
[2] wu f, wang j, wang y, kwok tt, kong sk, wong c. 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. |
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