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3PO | 6-Phosphosfructo-2-kinase (PFKFB3) inhibitor

3PO (18550-98-6) 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

References/Citations

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

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Catalog#  10-4609-0010

$45.00
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CAS:
18550-98-6
Catalog Number:
10-4609
Activity:
6-Phosphosfructo-2-kinase (PFKFB3) inhibitor
Chemical Name:
(2E)-3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
Molecular Weight:
210.23
Molecular Formula:
C13H10N2O
Solubility:
Soluble in DMSO (up to 15 mg/ml) or in Ethanol (up to 5 mg/ml)
Physical Properties:
Pale yellow solid
Purity:
99% by HPLC
NMR (Conforms)
Storage Temperature:
-20°C (des.)
Stability:
Stable for 1 year as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT
Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications.

Focus BiomoleculesPlymouth Meeting, PA USA1-855-FOCUS21

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