AZD-7545

Potent and selective pyruvate dehydrogenase kinase 2 (PDK2) inhibitor (IC50=6.4nM), consequently increasing pyruvate dehydrogenase (PDH) activity. Less potent inhibitor towards PDK1 and PDK3 (IC50=87 and 600nM, respectively). Inhibitor of glycolysis. Antiobesity and antidiabetic agent. Improves blood glucose control in obese (fa/fa) Zucker rats. Useful agent for immunometabolism research. To maintain a continuous and steady supply of ATP during the feed-fast cycle, cells must select fatty acid or glucose for fuel. This process is largely controlled by the pyruvate dehydrogenase complex (PDC), which regulates the entry of glycolytic products into the tricarboxylic acid cycle by catalyzing the oxidative decarboxylation of pyruvate to acetyl-coenzyme A (CoA) in the mitochondria of mammalian cells. PDKs and pyruvate dehydrogenase phosphatases (PDPs) are key regulators of PDC activity, and they act in a phosphorylation-dephosphorylation manner.