TEPP-46

TEPP-46 is a potent and selective small molecule activator of pyruvate kinase M2 (PKM2), a key glycolytic enzyme that is often upregulated in cancer cells. By binding allosterically at the dimer-dimer interface of PKM2, TEPP-46 stabilizes the active tetrameric form of the enzyme. This activation shifts cellular metabolism away from anabolic processes that support rapid cell proliferation and instead promotes catabolic energy production. In preclinical models, TEPP-46 has been shown to reduce tumor growth by interfering with cancer cell metabolism and to modulate immune responses by affecting T helper cell function. It has also demonstrated efficacy in mouse models of nonalcoholic steatohepatitis (NASH) by inhibiting disease progression through effects on liver macrophages (Kupffer cells)[1][7][9].

Other names

6-[(3-Aminophenyl)methyl]-4,6-dihydro-4-methyl-2-(methylsulfinyl)-5H-thieno[2',3':4,5]pyrrolo[2,3-d]pyridazin-5-one