KAN-0438757

KAN-0438757 (frequently misspelled as KAN-049757 in some literature) is a potent, selective, small-molecule inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3), a master regulator of glycolysis. Developed by Kancera in collaboration with the Karolinska Institutet, the compound was initially designed to target cancer cell metabolism and radiosensitize tumors by impairing homologous recombination (HR) DNA repair. More recently, KAN-0438757 has been investigated in cardiovascular and inflammatory models, where it normalizes endothelial glycolysis, reduces vascular inflammation, and mitigates myeloid-biased hematopoiesis in conditions like atherosclerosis and calcific aortic valve disease.