X4753
XCT790
≥98% (HPLC), ERRα agonist, solid
Synonym(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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About This Item
Empirical Formula (Hill Notation):
C23H13F9N4O3S
CAS Number:
Molecular Weight:
596.42
UNSPSC Code:
12352202
PubChem Substance ID:
NACRES:
NA.77
MDL number:
Product Name
XCT790, ≥98% (HPLC), solid
Quality Level
assay
≥98% (HPLC)
form
solid
color
yellow
solubility
DMSO: ≥10 mg/mL
storage temp.
2-8°C
SMILES string
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+
InChI key
HQFNFOOGGLSBBT-AWNIVKPZSA-N
Application
XCT790 has been used:
- as an estrogen-related receptor (ERR)α inverse agonist in C2C12 myotubes
- as an estrogen-related receptor (ERR)α inverse agonist to elucidate decidualization functionality of ERRα in endometrial embryonic stem cells
- as an autophagy inducer in human neuroblastoma SH-SY5Y and HeLa cell lines.
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).
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.
hcodes
pcodes
Hazard Classifications
Aquatic Chronic 4
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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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
G Vargas et al.
Oncogene, 38(7), 950-964 (2018-11-28)
Bone is the most common metastatic site for breast cancer. Estrogen-related-receptor alpha (ERRα) has been implicated in cancer cell invasiveness. Here, we established that ERRα promotes spontaneous metastatic dissemination of breast cancer cells from primary mammary tumors to the skeleton.
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
Global Trade Item Number
| SKU | GTIN |
|---|---|
| X4753-25MG | 04061833274873 |
| X4753-5MG | 04061837549762 |