ML-265

Potent and selective cell permeable pyruvate kinase M2 (PKM2) activator with little or no activity versus PKM1, PKL and PKR. Useful agent for immunometabolism research. Anticancer (reducing tumor sizes in mice) and anti-inflammatory agent. Shown to bind the enzyme PKM2 to promote formation of stable, enzymatically-active tetramers, thereby promoting the last rate-limiting step of glycolysis, converting PEP to pyruvate. In addition, it prevents PKM2 translocation to the nucleus resulting in reduced glycolysis and HIF-1alpha activation, causing diminished Warburg effect and IL-1beta production.