PFK15 (4382-63-2) 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. PFK15 inhibits PFKFB3 (IC50?= 207 nM) without inhibiting 96 other kinases.1?PFK15 was able to potently inhibit glucose and F26BP uptake. It induced apoptosis and reduced tumor growth?in vitro?and?in vivo.?PFK15 has been shown to inhibit tumor growth in various cancer models.2,3
PFK 15 is a novel inhibitor of glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3). It suppresses the glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and induces apoptosis in abnormal cells.
1) Clem?et al.?(2013),?Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer; Mol. Cancer Ther.?12?1461
2) Zhu?et al. (2016),?PFK15,a Small Molecule Inhibitor of PFKFB3, Induces Cell Cycle Arrest, Apoptosis and Inhibits Invasion in Gastric Cancer; PLoS One?11?e0163768
3) Li?et al. (2017),?Blockage of glycolysis by targeting PFKFB3 suppresses tumor growth and metastasis in head and neck squamous cell carcinoma; J. Exp. Clin. Cancer Res.?36?7
