Potent and selective activator of recombinant pyruvate kinase M2 (PKM2) with half-maximum activating concentration (AC50 value) of 92 nM, and little or no activity versus PKM1, PKL and PKR. Continuous dosing of mice with TEPP-46 decreased the development of human cancer cell xenografts, suggesting that increased pyruvate kinase activity can impair tumorigenesis.TEPP-46 can mimic the enzymatic properties of PKM1 in PKM2-expressing cells, alter cell metabolism, and induces changes in the kinetic properties of PKM2 that are identical to those induced by the endogenous PKM2 activator FBP.

KEYWORDS: TEPP-46 | Supplier | PKM2 activator | ML265 | TEPP46 | ML 265 | TEPP 46 | ML-265 | CAS [1221186-53-3] | Pyruvate | PKM2 | Activator | Enzymes |  Glycolysis | Warburg | tumorigenesis | cancer | glucose metabolism