PKM1 Kinase Inhibition Assay Kit

The PKM1 Kinase Inhibition Assay Kit is designed to measure the inhibition of human PKM1 (pyruvate kinase M1), also known as PKM1/M1 isoform, for screening and profiling applications using Kinase-Glo(R) Max as a detection reagent. The assay kit comes in a convenient 96-well and 384-well format, with enough purified PKM1, Phosphoenolpyruvate (PEP), ADP, and kinase assay buffer for 100 or 400 enzyme reactions. Need us to run inhibitor screens or profile your inhibitors against PKM1? Check out our Kinase Screening Services. PKM1 and PKM2 are different splicing products of the PKM gene, which catalyze the conversion of PEP (phosphoenolpyruvate) to pyruvate. The M1 isoform (PKM1) is expressed in muscle and brain, and the M2 isoform is expressed during embryogenesis, in adipose tissue and pancreatic islets, and is the predominant form found in cancer cells. PKM1 accounts for 90% of the metabolic activity in mature beta cells, and it is essential for PEP metabolism and insulin secretion. Studies have found that PKM1 can promote tumor growth in a cell-dependent context, by activating glucose catabolism and inducing autophagy/mitophagy. The development of therapeutics targeting PKM1 may thus prove beneficial in oncology, for example to treat SCLC (small-cell lung cancer).