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GW9662 is a potent antagonist of PPARγ with IC50 value of 3.3nM [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 20-30μM. 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].

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