PFK15 | Phosphofructo-2-kinase (PFKFB3) inhibitor

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

References/Citations

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