PKM2-IN-1 (Compound 3k) is a potent small molecule pyruvate kinase M2 (PKM2) inhibitor with IC50 of 2.95 uM, with less inhibition of PKM1 and PKL. PKM2-IN-1 (Compound 3k) shows nanomolar antiproliferative activity toward a series of cancer cell lines with high expression of PKM2 including HCT116, Hela and H1299 with IC50 values ranging from 0.18 to 1.56 μM. PKM2-IN-1 (Compound 3k) exhibits more cytotoxicity on cancer cells than normal cells.
