3PO

Pricing Availability   Qty
Cat.No. 5121 - 3PO | C13H10N2O | CAS No. 13309-08-5
Description: PFKFB3 inhibitor
Chemical Name: 3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
Purity: ≥99% (HPLC)
Datasheet
Citations
Reviews
Literature

Biological Activity

Originally reported to inhibit PFKFB3 (IC50 = 25 μM). More recent reports failed to demonstrate activity in a PFKFB3 kinase assay. Reduces glycolytic flux and suppresses glucose uptake. Inhibits endothelial cell proliferation and causes G2/M cell cycle arrest in vitro. Attenuates vessel sprouting and tumor growth in vivo. Amplifies the antiangiogenic effect of VEGFR blockade.

Technical Data

M. Wt 210.23
Formula C13H10N2O
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 13309-08-5
PubChem ID 5720233
InChI Key UOWGYMNWMDNSTL-ONEGZZNKSA-N
Smiles O=C(/C=C/C2=CN=CC=C2)C1=CC=NC=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 21.02 100

Preparing Stock Solutions

The following data is based on the product molecular weight 210.23. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 4.76 mL 23.78 mL 47.57 mL
5 mM 0.95 mL 4.76 mL 9.51 mL
10 mM 0.48 mL 2.38 mL 4.76 mL
50 mM 0.1 mL 0.48 mL 0.95 mL

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References

References are publications that support the biological activity of the product.

Clem et al (2008) Small-molecule inhibition of 6-phosphofructo-2-kinase activity suppresses glycolytic flux and tumor growth. Mol.Cancer Ther. 7 110 PMID: 18202014

Schoors et al (2014) Partial and transient reduction of glycolysis by PFKFB3 blockade reduces pathological angiogenesis. Cell Metab. 19 37 PMID: 24332967

Boyd et al (2015) Structure-based design of potent and selective inhibitors of the metabolic kinase PFKFB3. J.Med.Chem. 58 3611 PMID: 25849762


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Keywords: 3PO, 3PO supplier, PFKFB3, 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase, inhibitors, inhibits, glycolysis, antitumor, antitumour, antiangiogenic, Antiangiogenics, 5121, Tocris Bioscience

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