Pirinixic Acid (NSC 310038) is a synthetic thiacetic acid derivative used in biomedical research, carcinogenic Pirinixic acid is a peroxisome proliferator that activates specific peroxisome proliferator-activated receptors (PPAR).

PPARα:1.5 μM(EC50)

WY14643 significantly reduced visceral fat mass and total liver triglyceride content without increasing body weight. It enhanced systemic insulin sensitivity and improved insulin-mediated skeletal muscle glucose metabolism in both red (47%) and white (63%) muscle fibers, as well as in white adipose tissue (90%), while reducing muscle triglyceride and LCACoA accumulation. Administration of WY14643 (1 mg/kg i.v.) 30 minutes before left anterior descending artery occlusion led to a notable reduction in infarct size (~44%) in rats subjected to myocardial ischemia (25 minutes) followed by reperfusion (2 hours). In rats fed a high-fat diet, treatment with 3 mg/kg WY14643 lowered plasma glucose and triglyceride levels (-16% vs. untreated), leptin (-52%), muscle triglycerides (-34%), and overall long-chain acyl-coenzyme A (-41%) levels.

WY14643 (250 μM) significantly reduces the expression levels of VCAM-1, lowering it to 52% of those in human endothelial cells stimulated by TNF-α. At a concentration of 10 μM, WY 14643 acts on aortic smooth muscle cells to almost completely inhibit the production of IL-6 and prostaglandin induced by IL-1, as well as the expression of cyclooxygenase-2, through the suppression of the NF-κB signaling pathway. Pre-treating endothelial cells with WY 14643 (10 μM) before TNF-α stimulation decreases U937 cell adhesion by 50%.

Fluorescence Polarization Assay: Binding of HSP90 inhibitors to human full-length recombinant HSP90β is determined by a competitive binding fluorescence polarization assay, using a fluorescent pyrazole resorcinol probe.