Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2) without affecting PKM1 or pyruvate kinase-L (PKL), making it a potential anticancer agent [1].

Alkannin is a potent, specific inhibitor of PKM2, a crucial enzyme in the final rate-limiting step of glycolysis, essential for cancer cell proliferation and survival. It exhibits IC50 values of 0.3 μM without D-fructose-1,6-bisphosphate (FBP) and 0.9 μM with 125 μM FBP, indicating concentration-dependent inhibition of glycolytic flux in cancer cells expressing PKM2. Treatment with Alkannin (2.5-20 μM for 1 hour) reduces lactate production and glucose consumption in these cells [1]. Western Blot Analysis confirms that Alkannin (0-20 μM, 1 hour) significantly inhibits glycolytic rate in MCF-7 and A549 cell lines, which express PKM2 but not PKM1 and PKL [1].