SAICAR is an intermediate of de novo purine nucleotide biosynthesis, activates pyruvatekinase isoform M2 (PKM2) in an isozyme-selective manner (EC50: 0.3 mM).
ZINC08383544 is a specific pyruvatekinaseM2 activator which promotes the formation of PKM2 tetramer. ZINC08383544 effectively blocks PKM2 nuclear translocation, and inhibits the growth of tumor.
TLN-232, also known as CAP-232, is a synthetic cyclic heptapeptide with potential antineoplastic activity. Pyruvatekinase (PK) inhibitor TLN-232 targets pyruvatekinaseM2 (M2PK), which may disrupt tumor cell anaerobic glycolysis. M2PK is a dimeric isoform of PK and the predominant PK isoform found in tumor cells.