PKM2-IN-1

PKM2-IN-1 (also known as Compound 3k) is a selective, small-molecule inhibitor of pyruvate kinase M2 (PKM2) with an IC50 of 2.95 μM, exhibiting 4- to 5-fold selectivity over the PKM1 isoform. Discovered by researchers at Peking University, PKM2-IN-1 disrupts the PKM2 tetramer to promote monomer formation, thereby inhibiting its enzymatic activity. By blocking PKM2, the compound suppresses aerobic glycolysis (the Warburg effect), leading to reduced cell proliferation and increased apoptosis in various cancer models. Additionally, preclinical studies have demonstrated that PKM2-IN-1 significantly reduces cyst growth, inflammation, and fibrosis in mouse models of autosomal dominant polycystic kidney disease (ADPKD), highlighting its potential therapeutic utility in metabolic and hyperproliferative disorders.

Other names

(3-methyl-1,4-dioxonaphthalen-2-yl)methyl piperidine-1-carbodithioate1-Piperidinecarbodithioic acid, (1,4-dihydro-3-methyl-1,4-dioxo-2-naphthalenyl)methyl esterPyruvate Kinase M2 Inhibitor