Cat. No. 3928
Chemical Name: 3-[4-(2,4-Bis-trifluoromethylbenzyl
Biological ActivitySelective ERRα antagonist/inverse agonist (IC50 = ~400 nM). Displays no antagonist activity at ERRγ or ERα at concentrations below 10 μM. Interferes with PPARγ coactivator-1α (PGC-1α)/ERRα-dependent signaling: inhibits PGC-1α induction of ERRα and MAO-B gene expression and downregulates the constitutive transcriptional activity of ERRα in numerous cell lines.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Kong et al (2009) Peroxisome proliferator-activated receptor γ coactivator-1α enhances antiproliferative activity of 5'-deoxy-5-fluorouridine in cancer cells through induction of uridine phosphorylase. Mol.Pharmacol. 76 854. PMID: 19602572.
Lanvin et al (2007) Potentiation of ICI182,780 (Fulvestrant)-induced estrogen receptor-alpha degradation by the estrogen receptor-related receptor-α inverse agonist XCT790. J.Biol.Chem. 282 28328. PMID: 17631492.
Willy et al (2004) Regulation of PPARγ coactivator 1α (PGC-1α) signaling by an estrogen-related receptor alpha (ERRα) ligand. Proc.Natl.Acad.Sci.USA 101 8912.
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Citations are publications that use Tocris products. Selected citations for XCT 790 include:
Hwang et al (2014) Estrogen-related receptor α is required for efficient human cytomegalovirus replication. Proc Natl Acad Sci U S A 111 E5706. PMID: 25512541.
Teng et al (2014) Development of a stable cell line with an intact PGC-1α/ERRα axis for screening environmental chemicals. Mol Cancer 444 177. PMID: 24457025.
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Keywords: XCT 790, supplier, XCT790, ERRalpha, ERRa, ERRα, antagonists, inverse, agonists, PPARγ, PPARg, PPARgamma, coactivator-1α, coactivator-1alpha, coactivator-1a, PGC-1α, PGC-1alpha, PGC-1a, signaling, signalling, Tocris Bioscience, Estrogen and Related Receptor Antagonist products
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