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.
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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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