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.

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 .
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

• . 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.  [Content Brief]