pyruvate kinase m2

FX-11 (LDHA Inhibitor FX11) is A potent, selective and competitive specific inhibitor of lactate dehydrogenase A (LDHA) with a Ki of 8 μM. FX-11 can activate PKM2 (pyruvate kinase M2). FX-11 can reduce ATP levels, induce oxidative stress and ROS production, and cause cell death. FX-11 appeared antitumor activity during xenotransplantation of lymphoma and pancreatic cancer.

DL-Serine is a non-essential amino acid and a natural ligand and allosteric activator of pyruvate kinase M2.

DASA-58 is a specific and potent Pyruvate kinase M2 (PKM2) activator.

TEPP-46 (ML265) is an activator of pyruvate kinase M2 (PKM2) (AC50=92 nM), selective for PKM1, PKL and PKR. TEPP-46 has antitumor activity.

SAICAR, an intermediate of de novo purine nucleotide biosynthesis, selectively activates pyruvate kinase isoform M2 (PKM2) with an EC50 of 0.3 mM.

PKM2-IN-8 (Compound 9b) is an inhibitor of pyruvate kinase M2 (PKM2) with an IC50 of 0.31 μM. It exhibits potent antiproliferative activity against U87MG glioma cells. PKM2-IN-8 induces early apoptosis and reduces lactate levels. This compound is useful for research in glioblastoma.

Alkannin is a potent and specific inhibitor of tumor-specific pyruvate kinase-M2 (PKM2) without affecting PKM1 or pyruvate kinase-L (PKL), making it a potential anticancer agent [1].

PKM2 activator 2, with an AC50 value of 66 nM, is a pyruvate kinase M2 (PKM2) activator that demonstrates anti-tumor proliferative properties and attenuates the Warburg effect by normalizing cellular glycolytic metabolism through the activation of PKM2.

ZINC08383544 is a specific pyruvate kinase M2 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. Pyruvate kinase (PK) inhibitor TLN-232 targets pyruvate kinase M2 (M2PK), which may disrupt tumor cell anaerobic glycolysis. M2PK is a dimeric isoform of PK and the predominant PK isoform found in tumor cells.

PF-06284674 is a cell permeable, potent and selective M2 isoform of pyruvate kinase (PKM2) activator.

ML202 is a highly specific allosteric activator of human pyruvate kinase M2 (hPK-M2), enhancing the cooperativity of phosphoenolpyruvate (PEP) binding with negligible effect on adenosine diphosphate (ADP) binding.