PKM2-IN-1

94164-88-2

C18H19NO2S2

H2O : < 0.1 mg/mL (insoluble); DMSO : 5.56 mg/mL (16.09 mM; Need ultrasonic)

Metabolic Enzyme/Protease

PKM2-IN-1 is a pyruvate kinase M2 (PKM2) inhibitor with an IC₅₀ of 2.95 uM. IC50 & Target: IC50: 2.95 uM (PKM2)^[1] In Vitro: PKM2-IN-1 is a pyruvate kinase M2 (PKM2) inhibitor with an IC₅₀ of 2.95+/-0.53 uM. Results show that most of the tested compounds exhibit some degree of PKM2 inhibition and some compounds, such as PKM2-IN-1 (compound 3k) and 6d, display more potent activity than the positive control shikonin. The representative compounds PKM2-IN-1, 6d display dose-dependent inhibition of PKM2 with less inhibition of PKM1 and PKL like shikonin. Among all tested compounds, the most potent compounds are 3a, PKM2-IN-1 and 3r, which exhibit IC₅₀ values against HCT116 and Hela cells ranging from 0.39 to 0.41 uM, 0.18 to 0.29 uM and 0.18 to 0.38 uM, respectively^[1].