3PO Struktur

3PO

Bezeichnung:3PO

CAS-Nr18550-98-6

Englisch Name:3PO

CBNumberCB33121068

SummenformelC13H10N2O

Molgewicht210.23

MOL-Datei18550-98-6.mol

3PO physikalisch-chemischer Eigenschaften

Siedepunkt	387.8±42.0 °C(Predicted)
Dichte	1.192±0.06 g/cm3(Predicted)
storage temp.	2-8°C
Löslichkeit	Soluble in DMSO (up to 15 mg/ml) or in Ethanol (up to 5 mg/ml)
pka	3.49±0.11(Predicted)
Aggregatzustand	powder
Farbe	white to beige
Stabilität	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.

Gefahreninformationscode (GHS)

3PO Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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
Definition
ChEBI: 3PO is a member of the class of pyridines that is pyridine substituted by a 3-oxo-3-(pyridin-4-yl)prop-1-en-1-yl group at position 3. An inhibitor of PFKFB3 kinase, an enzyme with a key role in glycolysis. It has a role as an antineoplastic agent, an angiogenesis inhibitor, an autophagy inducer, an apoptosis inducer and an EC 2.7.1.105 (6-phosphofructo-2-kinase) inhibitor. It is a member of pyridines and an enone.
Biochem/physiol Actions
3PO is a potent and selective inhibitor of PFKFB3 (6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase) that reduces glycolytic flux and suppresses glucose uptake. 3PO is selectively cytostatic to transformed cells and suppresses the growth of established tumor in mice.
Einzelnachweise
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

3PO Upstream-Materialien And Downstream Produkte

3PO Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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