GW-9662 (22978-25-2) is a selective PPARγ antagonist (IC50 = 3.3, 32 and 2000 nM for PPARγ, PPARα and PPARδ respectively)1. Blocks the inhibition of osteoclast formation induced by IL-4 (1-2 μM)2. Displays anticancer activity inhibits growth of human mammary tumor cell lines3. GW-9662 is a useful tool for dissecting the involvement of PPARγ in cellular physiology4,5.
1) Leesnitzer et al. (2002), Functional consequences of cysteine modification in the ligand binding sites of peroxisome proliferator activated receptors by GW9662; Biochemistry, 41 6640
2) Bendixen et al. (2001), IL-4 inhibits osteoclast formation through a direct action on osteoclast precursors via peroxisome proliferator-activated receptor gamma 1; Proc. Natl. Acad. Sci. USA, 98 2443
3) Seargent et al. (2004), GW9662, a potent antagonist of PPARgamma inhibits growth of breast cancer tumour cells and promotes the anticancer effects of the PPARgamma agonist rosiglitazone, independently of PPARgamma activation; Br. J. Pharmacol., 143 933
4) Cheng et al. (2014), β-Caryophyllene Ameliorates the Alzheimer-Like Phenotype in APP/PS1 Mice through CB2 Receptor Activation and the PPARγ Pathway; Pharmacology, 94 1
5) Liu et al. (2014), Curcumin protects neurons against oxygen-glucose deprivation/reoxygenation-induced injury through activation of peroxisome proliferator-activated-γ function; J. Neuro. Sci. Res., 92 1549