PKM2 Kinase Inhibition Assay Kit

The PKM2 Kinase Inhibition Assay Kit is designed to measure the inhibition of human PKM2 (pyruvate kinase M2), also known as PKM1/M2 isoform a, for screening and profiling applications using Kinase-Glo(R) Max as a detection reagent. The assay kit comes in a convenient 96-well format or 384-well format, with enough purified PKM2, Phosphoenolpyruvate (PEP), ADP, allosteric PKM2 activator FBP (fructose-1,6-bisphosphate), and kinase assay buffer for 100 or 400 enzyme reactions. Need us to run inhibitor screens or profile your inhibitors against PKM2? Check out our Kinase Screening Services. PKM2 (pyruvate kinase M2), also known as PKM1/M2 isoform a, is an isoenzyme of the glycolytic enzyme pyruvate kinase family. It is found in differentiated tissues, including lung cells, fat tissue, and cells that require a high rate of acid nucleic synthesis, such as cancer cells. PKM2 can form either highly active tetramers or low-activity dimers. The dimeric form slows glycolysis, diverting glucose metabolism from oxidative phosphorylation toward lactate production - a hallmark of tumor cells. This low-activity dimer is strongly associated with cancer because it channels glucose intermediates into biosynthetic pathways that support cell growth. PKM2 Inhibitors target the low-activity dimeric form of PKM2 that supports cancer cell survival by enhancing glycolysis and biosynthetic pathways. Inhibitors have demonstrated effectiveness in sensitizing cancer cells to chemotherapy. The dual impact on metabolism and transcription makes PKM2 inhibitors attractive candidates for combination cancer therapies.