GW-9662
PPARγ antagonist / 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. A useful tool for dissecting the involvement of PPARγ in cellular physiology4,5.
Biochemicals & reagents
22978-25-2
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), ß-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
RT
TARGET: Transcription factor -- PATHWAY: Cytokine; PPAR; Transcription; Glycation -- RESEARCH AREA: Angiogenesis -- DISEASE AREA: Cancer; InflammationDiabetes; Atherosclerosis