3PO

3PO (18550-98-6) is an inhibitor of the metabolic enzyme 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3). PFKFB3 is constitutively expressed by neoplastic cells and is required for the high glycolytic rate (Warburg Effect) of these cells. 3PO inhibits PFKFB3 (IC50= 1.4 – 24 μM for various cancer cell lines), suppresses glucose uptake, and lowers intracellular concentrations of Fru-2,6-BP, lactate, ATP, NAD+, and NADH.1 Inhibition of cancer cell metabolism via blocking the action of PFKFB3 has been studied in various models.2-4 Inhibition of PFKFB3 has been shown to induce autophagy as a survival mechanism in cancer cells.5 3PO has also been used to reduce pathological angiogenesis.6

ChEBI: 3PO is a member of the class of pyridines that is pyridine substituted by a 3-oxo-3-(pyridin-4-yl)prop-1-en-1-yl group at position 3. An inhibitor of PFKFB3 kinase, an enzyme with a key role in glycolysis. It has a role as an antineoplastic agent, an angiogenesis inhibitor, an autophagy inducer, an apoptosis inducer and an EC 2.7.1.105 (6-phosphofructo-2-kinase) inhibitor. It is a member of pyridines and an enone.

3PO is an inhibitor of PFKFB3. 3PO attenuates the proliferation of several cancer cell lines with IC50s of 1.4-24 μmol/L. 3PO suppresses glucose uptake and decreases the intracellular concentration of Fru-2,6-BP, lactate, ATP, NAD+ and NADH. 3PO can be used for the research of cancer[1].