3PO

SKU:

10-4609-10mg

CAS Number:

18550-98-6

Extra Details:

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

Molecular Weight:

210.23

Physical State:

Pale yellow solid

References:

1) Clem et al. (2008), Small-molecule inhibition of 6-phosphofructo-2-kinase activity suppresses glycolytic flux and tumor growth; Mol.Cancer Ther. 7 110 2) Clem et al. (2013), Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer; Mol.Cancer Ther. 12 1461 3) Lea et al. (2015), Inhibition of Growth of Bladder Cancer Cells by 3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one in Combination with Other Compounds Affecting Glucose Metabolism; Anticancer Res. 35 5889 4) Lea et al. (2016), Inhibition of Growth by Combined Treatment with Inhibitors of Lactate Dehydrogenase and either Phenformin or Inhibitors of 6-Phosphofructo-2-kinase/Fructose-2,6-bisphosphatae 3; Anticancer Res. 36 1479 5) Klarer et al. (2014), Inhibition of 6-phosphofructo-2-kinase (PFKFB3) induces autophagy as a survival mechanism; Cancer Metab. 2 2 6) Schoors et al. (2014), Partial and transient reduction of glycolysis by PFKFB3 blockade reduces pathological angiogenesis; Cell Metab. 19 37

Shipping Conditions:

Ambient

Storage Conditions:

-20°C

Supplier:

Focus Biomolecules

• Manufacturer's Data Sheet:

Purity:

99% by HPLC, NMR (Conforms)

Chemical Name:

(2E)-3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one