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3PO is a novel small-molecule inhibitor of the PFKFB3 isozyme, attenuates the proliferation of several human malignant hematopoietic and adenocarcinoma cell lines with IC50 of 1.4-24 μM. 3PO reduces glycolytic flux and suppresses glucose uptake. 3PO inhibits endothelial cell proliferation and causes G2/M cell cycle arrest in vitro. 3PO attenuates vessel sprouting and tumor growth in vivo. 3PO amplifies the antiangiogenic effect of VEGFR blockade.
| Cell Experiment | |
|---|---|
| Cell lines | HUVECs |
| Preparation method | Cells were seeded in gelatin-coated 96 well plates at a density of 4 x10^4 cells/cm2 and cultured for 24 hours before stimulation with IL-1β (1ng/ml) in the presence or absence of 3PO (20 μM, IC50 = 22.9 μM) or YN1 (20 μM, IC50 0.67 μM) for 3 hours |
| Concentrations | 20 μM |
| Incubation time | 3 hours |
| Animal Experiment | |
|---|---|
| Animal models | C57BL/6 mice |
| Formulation | 3PO in 50 μL DMSO and only vehicle DMSO |
| Dosages | 0.07 mg/g |
| Administration | Intragastric administration 0 and 6 h after CLP |
| Molecular Weight | 210.23 |
| Formula | C13H10N2O |
| CAS Number | 18550-98-6 |
| Solubility (25°C) | DMSO 21.02 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related PFKFB3 Products |
|---|
| PFK-015
PFK-015 is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor. PFK-015 inhibits recombinant PFKFB3 with an IC50 value of 110 nM and inhibits PFKFB3 activity in cancer cells with an IC50 value of 20 nM. |
| PFK-158
PFK-158, also known as ACT-PFK-158, is a potent and selective inhibitor of 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatases (PFK-2/FBPase) isoform 3 (PFKFB3) with potential antineoplastic activity. |
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