Cat. No. 1508
Chemical Name: 2-Chloro-5-nitro-N-phenylbenzamide
Biological ActivitySelective PPARγ antagonist (IC50 values are 3.3, 32 and 2000 nM for PPARγ, PPARα and PPARδ respectively). Blocks the inhibition of osteoclast formation induced by IL-4 in the low micromolar range (1-2 μM), therefore is more potent than BADGE (Cat. No. 1326). Anticancer, inhibits growth of human mammary tumor 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 / Product Datasheet / Safety Data Sheet
Seargent et al (2004) GW9662, a potent antaognist of PPARγ, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARγ agonist rosiglitazone, independently of PPARγ activation. Br.J.Pharmacol. 143 933. PMID: 15533890.
Leesnitzer et al (2002) Functional consequences of cysteine modification in the ligand binding sites of peroxisone proliferator activated receptors by GW9662. Biochemistry 41 6640. PMID: 12022867.
Bendixen et al (2001) IL-4 inhibits osteoclast formation through a direct action on osteoclast precursors via peroxisome proliferator-activated receptor γ1. Proc.Natl.Acad.Sci.U.S.A. 98 2443. PMID: 11226258.
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Citations are publications that use Tocris products. Selected citations for GW 9662 include:
Mottillo et al (2012) Lipolytic products activate peroxisome proliferator-activated receptor (PPAR) α and δ in brown adipocytes to match fatty acid oxidation with supply. PLoS One 287 25038. PMID: 22685301.
Ramachandran et al (2012) Isorhamnetin inhibits proliferation and invasion and induces apoptosis through the modulation of peroxisome proliferator-activated receptor γ activation pathway in gastric cancer. J Biol Chem 287 38028. PMID: 22992727.
Scuderi et al (2012) Palmitoylethanolamide exerts neuroprotective effects in mixed neuroglial cultures and organotypic hippocampal slices via peroxisome proliferator-activated receptor-α. Arterioscler Thromb Vasc Biol 9 49. PMID: 22405189.
Esposito et al (2011) Cannabidiol reduces Aβ-induced neuroinflammation and promotes hippocampal neurogenesis through PPARγ involvement. FASEB J 6 e28668. PMID: 22163051.
Ali et al (2009) Antiplatelet actions of statins and fibrates are mediated by PPARs. J Neurosci 29 706. PMID: 19150877.
Ali et al (2006) Role of nuclear receptor signaling in platelets: antithrombotic effects of PPARβ. J Neuroinflammation 20 326. PMID: 16368717.
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Keywords: GW 9662, supplier, Selective, PPARγ, PPARgamma, antagonists, Peroxisome, Proliferator-activating, Receptors, PPAR, GW9662, Tocris Bioscience, PPARγ Antagonist products