Chemical Name: 1-(4-Pyridinyl)-3-(2-quinolinyl)-2-propen-1-one
Biological ActivityOriginally reported to be a selective PFKFB3 inhibitor (IC50 = 207 nM); a more recent report failed to demonstrate activity in a PFKFB3 kinase assay. Selective for PFKFB3 over a panel of 96 kinases. Reduces glucose uptake and induces apoptosis in H522 lung adenocarcinoma and Jurkat T cell leukemia cells. Suppresses glucose uptake and tumor growth, and inhibits metastasis of Lewis lung carcinoma cell xenografts in mice.
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.
Targeting the Warburg effect in cancer; relationships for 2-arylpyridazinones as inhibitors of the key glycolytic enzyme 6-phosphofructo-2-kinase/2,6-bisphosphatase 3 (PFKFB3).
Brooke et al.
Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer.
Clem et al.
Mol.Cancer Ther., 2013;12:1461
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