X4753
XCT790
≥98% (HPLC), solid
Synonyme(s) :
3-[4-(2,4-Bis-trifluoromethylbenzyloxy)-3-methoxyphenyl]-2-cyano-N-(5-trifluoromethyl-1,3,4-thiadiazol-2-yl)acrylamide
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201.00 CHF
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770.00 CHF
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5 MG
201.00 CHF
25 MG
770.00 CHF
About This Item
Formule empirique (notation de Hill) :
C23H13F9N4O3S
Numéro CAS:
Poids moléculaire :
596.42
Numéro MDL:
Code UNSPSC :
12352202
ID de substance PubChem :
Nomenclature NACRES :
NA.77
Produits recommandés
Niveau de qualité
Essai
≥98% (HPLC)
Forme
solid
Couleur
yellow
Solubilité
DMSO: ≥10 mg/mL
Température de stockage
2-8°C
Chaîne SMILES
COc1cc(ccc1OCc2ccc(cc2C(F)(F)F)C(F)(F)F)\C=C(/C#N)C(=O)Nc3nnc(s3)C(F)(F)F
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+
Clé InChI
HQFNFOOGGLSBBT-AWNIVKPZSA-N
Application
XCT790 has been used:
- as an estrogen-related receptor (ERR)α inverse agonist in C2C12 myotubes[1]
- as an estrogen-related receptor (ERR)α inverse agonist to elucidate decidualization functionality of ERRα in endometrial embryonic stem cells[2]
- as an autophagy inducer in human neuroblastoma SH-SY5Y and HeLa cell lines. [3]
Actions biochimiques/physiologiques
XCT 790 is a 5′adenosine monophosphate-activated protein kinase (AMPK) activator.[4] It also acts as a proton ionophore and an uncoupler of oxidative phosphorylation in mitochondria.[4] XCT790 impairs vascular endothelial growth factor (VEGF) and angiopoietin 2 (Ang-2) expression[5] and exhibits suppression of endometrial tumor via estrogen-related receptor (ERRα) inhibition.[6] XCT790 mediates cell cycle arrest and favors apoptosis in triple-negative breast cancer (TNBC).[7]
XCT790 is a potent and specific inverse agonist of ERRα. Selective; showing no significant antagonist activity on related nuclear receptors, such as ERRγ or ERα at concentrations below 10 μM.
XCT790 is a potent and specific inverse agonist of ERRα. XCT790 is selective; showing no significant antagonist activity on related nuclear receptors, such as ERRγ or ERα at concentrations below 10 μM. XCT790 inhibits the constitutive activity of ERRα in both biochemical and cell-based assays. The IC50 value is 300-500 nM in transient transfection assays using GAL4-ERR LBD or full-length ERR with the mSHP promoter.
Mentions de danger
Conseils de prudence
Classification des risques
Aquatic Chronic 4
Code de la classe de stockage
11 - Combustible Solids
Classe de danger pour l'eau (WGK)
WGK 3
Point d'éclair (°F)
Not applicable
Point d'éclair (°C)
Not applicable
Équipement de protection individuelle
Eyeshields, Gloves, type N95 (US)
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Ying-Min Wu et al.
Oncotarget, 7(11), 12568-12581 (2016-02-13)
There is an urgent clinical need for targeted therapy approaches for triple-negative breast cancer (TNBC) patients. Increasing evidences suggested that the expression of estrogen-related receptor alpha (ERRα) was correlate with unfavorable clinical outcomes of breast cancer patients. We here show
Rasmus J O Sjögren et al.
Diabetologia, 64(9), 2077-2091 (2021-06-17)
Increased levels of branched-chain amino acids (BCAAs) are associated with type 2 diabetes pathogenesis. However, most metabolomic studies are limited to an analysis of plasma metabolites under fasting conditions, rather than the dynamic shift in response to a metabolic challenge.
Banu Eskiocak et al.
Biochemistry, 53(29), 4839-4846 (2014-07-08)
XCT 790 is widely used to inhibit estrogen-related receptor α (ERRα) activity as an inverse agonist. Here, we report that XCT 790 potently activates AMP kinase (AMPK) in a dose-dependent and ERRα-independent manner, with active concentrations more than 25-fold below
Sin-Aye Park et al.
British journal of cancer, 123(6), 988-999 (2020-06-24)
Gremlin-1 (GREM1), one of the bone morphogenetic protein antagonists, is involved in organogenesis, tissue differentiation and kidney development. However, the role of GREM1 in cancer progression and its underlying mechanisms remain poorly understood. The role of GREM1 in breast cancer
PengMing Sun et al.
Cancer management and research, 10, 2521-2535 (2018-08-22)
To explore the targeted therapy of estrogen-related receptor α (ERRα) in endometrial cancer (EC) cells and its potential mechanisms. The mRNA and protein expression levels of ERRα and estrogen receptor α (ERα) were detected by qPCR and Western blotting in
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