3PO

3PO is a competitive inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphate 3 (PFKFB3; IC₅₀ = 23 µM) that causes a rapid reduction in fructose-2,6-bisphosphate (F2,6BP), glucose uptake, and lactate secretion.^1,2 This is followed by a reduction in the steady-state concentration of ATP and NADH, resulting in cell cycle arrest in Jurkat T cell leukemia cells.^1,2 3PO is selectively cytostatic to ras-transformed bronchial epithelial cells relative to normal bronchial epithelial cells.¹ 3PO markedly reduces intracellular F2,6BP, glucose uptake, and growth of established tumors in mice.¹ It also blocks angiogenesis, reducing vessel sprouting in endothelial cell spheroids, zebrafish embryos, and the postnatal mouse retina by inhibiting endothelial cell proliferation and migration.³

WARNING This product is not for human or veterinary use.

1. Clem, B., Telang, S., Clem, A., et al. Small-molecule inhibition of 6-phosphofructo-2-kinase activity suppresses glycolytic flux and tumor growth. Mol. Cancer Ther. 7(1), 110-120 (2008).

2. Clem, B.F., O'Neal, J., Tapolsky, G., et al. Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer. Mol. Cancer Ther. 12(8), 1461-1470 (2013).

3. Schoors, S., De Bock, K., Cantelmo, A.R., et al. Partial and transient reduction of glycolysis by PFKFB3 blockade reduces pathological angiogenesis. Cell Metab. 19(1), 37-48 (2014).