Alkannin is a potent and specific tumor-specific pyruvate kinase-M2 (PKM2) inhibitor that does not inhibit PKM1 and pyruvate kinase-L (PKL). Alkannin is a potential anticancer agent [1].

Alkannin is a potent and specific inhibitor to PKM2, an enzyme that dictates the last rate-limiting step of glycolysis, which is essential for cancer cells’ proliferation and survival. In the absence of D-fructose-1,6-bisphosphate (FBP), the IC 50 of Alkannin is 0.3 μM. In the presence of FBP (125 μM), the IC 50 of Alkannin is 0.9 μM, respectively. Alkannin effectively inhibits the cellular glycolytic flux in cancer cells dominantly expressing PKM2 [1]. Alkannin (2.5-20 μM, 1 hour) inhibit the rates of cellular lactate production and glucose consumption [1]. Western Blot Analysis [1] Cell Line: MCF-7 and A549 express PKM2 but not PKM1 and PKL Concentration: 0-20 μM Incubation Time: 1 hour Result: Inhibited the cellular glycolytic rate in a concentration-dependent manner.