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

CAS:
18550-98-6
Catalog Number:
10-4609
Activity:
6-Phosphofructo-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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Available Options

Size :PriceQuantity 
10 mg$45.00
50 mg$170.00

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

CAS:
18550-98-6
Catalog Number:
10-4609
Activity:
6-Phosphofructo-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
Stability:
Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months.
Shipping Code:
RT

Safety Data Sheet:

N/A

Product Data Sheet:

Materials provided by Focus Biomolecules are for laboratory research use only and are not intended for human or veterinary applications. Please note that we do not sell to individuals and that all orders placed by non-research organizations will incur a $20 restocking/refund fee

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