PKM2 activator 2

PKM2 activator 2 is a pyruvate kinase M2 (PKM2) activitor with an AC50 value of 66 nM. PKM2 activator 2 may show anti-tumor proliferation effect and relieve the Warburg effect, while PKM2 activation can restore normal glycolytic metabolism in cells[1].

Research Areas >> Cancer

PKM2:66 nM (EC50)

PKM2 leads to increased availability of glycolyctic intermediates for biosynthesis of amino acids, nucleic acids, and lipid building blocks for cellular construction in cancer cells. However, PKM2 shows down-regulated expression and dimeric form in tumors and cancer cell lines [1]. PKM2 activator 2 (compound 28) is a highly potent activator, activates pyruvate kinase with an AC50 value of 66 nM in the luciferase-coupled assay[1].

[1]. Boxer MB, et al. Evaluation of substituted N,N'-diarylsulfonamides as activators of the tumor cell specific M2 isoform of pyruvate kinase. J Med Chem. 2010 Feb 11;53(3):1048-55.