纯度:99% by HPLC,;NMR (Conforms)
分子式:C13H10N2O
分子量:210.23
溶剂:DMSO (15 mg/ml) Ethanol (5 mg/ml)
性状:Pale yellow solid
存储:-20°C
Activity (short version):6-Phosphofructo-2-kinase (PFKFB3) inhibitor
Function / Pharmacology:3PO 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