GW9662

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Background

GW9662 is a potent antagonist of PPARγ with IC50 value of 3.3 nM [1].
PPARγ belongs to the nuclear receptor superfamily, the inhibition of it is a strategy for treatment of several cancers, including breast. GW9662 acts as a potent, irreversible and selective PPARγ antagonist in both cell-free and cell-based assays. It modifies a cysteine residue in the ligand-binding site of PPARγ. In three breast cell lines including MCF7, MDA-MB-231 and MDA-MB-468, GW9662 suppresses the cell viability with IC50 values ranging from 20-30 μM. In addition, GW9662 is reported to abolish the protection of LPS in a model of renal ischemia/reperfusion (I/R). In this model, the renal/glomerular dysfunction, tubular dysfunction and reperfusion injury caused by I/R can be significantly attenuated by LPS, and administration of GW9662 reverses this [2, 3].

[1] Fong WH, Tsai HD, Chen YC, Wu JS, Lin TN. Anti-apoptotic actions of PPAR-gamma against ischemic stroke. Mol Neurobiol. 2010 Jun; 41 (2-3): 180-6.
[2] Seargent JM, Yates EA, Gill JH. GW9662, a potent antagonist of PPARgamma, inhibits growth of breast tumour cells and promotes the anticancer effects of the PPARgamma agonist rosiglitazone, independently of PPARgamma activation. Br J Pharmacol. 2004 Dec; 143 (8): 933-7.
[3] Collino M, Patel NS, Lawrence KM, Collin M, Latchman DS, Yaqoob MM, Thiemermann C. The selective PPARgamma antagonist GW9662 reverses the protection of LPS in a model of renal ischemia-reperfusion. Kidney Int. 2005 Aug; 68 (2): 529-36.