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GW 9662
- Soluble in DMSO and EtOH
- MF: C13H9ClN2O3
- MW: 276.68
Description
GW 9662 is a potent PPARγ antagonist with IC50 values of 3.3 nM, 32 nM and 2000 nM for PPARγ, PPARα and PPARδ, respectively. It is widely used to define PPARγ-dependent and PPARγ-independent effects in cancer, angiogenesis and inflammatory injury models.
PPARγ regulates adipogenesis, metabolism, inflammation and cellular differentiation. GW 9662 is a valuable nuclear-receptor probe for dissecting PPAR subtype selectivity, PPARγ antagonist pharmacology and context-dependent effects of PPARγ ligands.
Key Features
- Potent PPARγ antagonist
- IC50: 3.3 nM at PPARγ
- Selectivity over PPARα and PPARδ
- Useful for separating PPARγ-dependent from independent mechanisms
Applications
- PPARγ pharmacology
- Nuclear receptor signaling assays
- Cancer and angiogenesis studies
- Metabolic and inflammatory pathway research
More Information
| Parent CAS No. | 22978-25-2 |
|---|---|
| Chemical Name | 2-chloro-5-nitro-N-phenylbenzamide |
| SMILES | C1([N+]([O-])=O)C=C(C(=O)NC2C=CC=CC=2)C(Cl)=CC=1 |
| MFCD | MFCD01215270 |
| InChi | InChI=1S/C13H9ClN2O3/c14-12-7-6-10(16(18)19)8-11(12)13(17)15-9-4-2-1-3-5-9/h1-8H,(H,15,17) |
| InChiKey | DNTSIBUQMRRYIU-UHFFFAOYSA-N |
| CID | 644213 |
| Short Description | PPARγ antagonist |
References
- U. Krause et al. Pharmaceutical modulation of canonical Wnt signaling in multipotent stromal cells for improved osteoinductive therapy. PNAS USA 2010, 107, 4147-4152.
- J.M. Seargent et al. GW9662, a potent antagonist 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. 2004, 143, 933-937.
- M. Collino et al. The selective PPARgamma antagonist GW9662 reverses the protection of LPS in a model of renal ischemia-reperfusion. Kidney Int. 2005, 68, 529-536.
- L.M. Leesnitzer et al. Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662. Biochem. 2002, 41, 6640-6650.
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