Catalog Number: 5121
Chemical Name: 3-(3-Pyridinyl)-1-(4-pyridinyl)-2-propen-1-one
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
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
    >99%
  • Storage:
    Store at -20°C
  • CAS No:
    13309-08-5
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.
Background References
  1. Small-molecule inhibition of 6-phosphofructo-2-kinase activity suppresses glycolytic flux and tumor growth.
    Clem et al.
    Mol.Cancer Ther., 2008;7:110
  2. Partial and transient reduction of glycolysis by PFKFB3 blockade reduces pathological angiogenesis.
    Schoors et al.
    Cell Metab., 2014;19:37
  3. Structure-based design of potent and selective inhibitors of the metabolic kinase PFKFB3.
    Boyd et al.
    J.Med.Chem., 2015;58:3611

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