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Documenti fondamentali

SML1343

Sigma-Aldrich

3PO

≥98% (HPLC)

Sinonimo/i:

(2E)-3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one, 3PO (inhibitor of glucose metabolism)

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About This Item

Formula empirica (notazione di Hill):
C13H10N2O
Numero CAS:
Peso molecolare:
210.23
Numero MDL:
Codice UNSPSC:
12352200
ID PubChem:
NACRES:
NA.77

Livello qualitativo

Saggio

≥98% (HPLC)

Stato

powder

Colore

white to beige

Solubilità

DMSO: 5 mg/mL, clear (warmed)

Temperatura di conservazione

2-8°C

Stringa SMILE

O=C(C1=CC=NC=C1)/C=C/C2=CN=CC=C2

InChI

1S/C13H10N2O/c16-13(12-5-8-14-9-6-12)4-3-11-2-1-7-15-10-11/h1-10H/b4-3+
UOWGYMNWMDNSTL-ONEGZZNKSA-N

Applicazioni

3PO has been used as a 6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase isoform 3(PFKFB3) inhibitor to study its effect on cell viability loss, apoptosis, and necroptosis in colorectal cancer cells. It has also been used as a PFKFB3 inhibitor to inhibit glycolysis and study its effects on cell viability and reactive oxygen species (ROS) production in trabectedin (TRB) and lurbinectedin (LUR) treated human macrophages (hMFs).

Azioni biochim/fisiol

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.
3PO is a potent and selective inhibitor of PFKFB3 (6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase).
Inhibition of glycolysis by PFKFB3 blockade mediated by 3PO reduced pathological angiogenesis in cancer and inflammation. 3PO aids in the regulation of endothelial proliferation and migration. It also reduces pro-inflammatory activation of endothelial cells and experimental inflammation in vivo. Therefore, it may be a potential therapeutic for treating chronic inflammation. Its anti-inflammatory activity in human endothelial cells is independent of its target PFKFB3.

Codice della classe di stoccaggio

11 - Combustible Solids

Classe di pericolosità dell'acqua (WGK)

WGK 3

Punto d’infiammabilità (°F)

Not applicable

Punto d’infiammabilità (°C)

Not applicable


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American journal of cancer research, 11(5), 2062-2080 (2021-06-08)
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Anticancer research, 40(5), 2613-2625 (2020-05-06)
The occurrence of BRAFV600E mutation causes an up-regulation of the B-raf kinase activity leading to the stabilization of hypoxia-inducible factor 1-alpha (HIF-1α) - the promoter of the 6-phosphofructo-2-kinase/fructose-2,6-biphosphatase 3 (PFKFB3) enzyme. The aim of the study was to examine the
Husniye Kantarci et al.
eLife, 9 (2020-04-28)
Recent studies indicate that many developing tissues modify glycolysis to favor lactate synthesis (Agathocleous et al., 2012; Bulusu et al., 2017; Gu et al., 2016; Oginuma et al., 2017; Sá et al., 2017; Wang et al., 2014; Zheng et al.
Adrián Povo-Retana et al.
Cancers, 12(10) (2020-10-24)
Tumor-associated macrophages (TAMs) play a crucial role in suppressing the immunosurveillance function of the immune system that prevents tumor growth. Indeed, macrophages can also be targeted by different chemotherapeutic agents improving the action over immune checkpoints to fight cancer. Here

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