SML1343
3PO
≥98% (HPLC)
Sinónimos:
(2E)-3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one, 3PO (inhibitor of glucose metabolism)
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About This Item
Fórmula empírica (notación de Hill):
C13H10N2O
Número de CAS:
Peso molecular:
210.23
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
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Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 5 mg/mL, clear (warmed)
storage temp.
2-8°C
SMILES string
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+
InChI key
UOWGYMNWMDNSTL-ONEGZZNKSA-N
Application
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).
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.
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.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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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
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