A selective inhibitor of PFKFB3
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PFK15

Item No. 17689

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-(4-pyridinyl)-3-(2-quinolinyl)-2-propen-1-one
CAS Number
4382-63-2
Molecular Formula
C17H12N2O
Formula Weight
260.3
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMF:PBS (pH 7.2) (1:3): 0.25 mg/mlDMSO: 10 mg/mlEthanol: 1 mg/ml
λmax
232, 278, 330 nm
SMILES
O=C(C1=CC=NC=C1)/C=C/C2=NC3=CC=CC=C3C=C2
InChi Code
InChI=1S/C17H12N2O/c20-17(14-9-11-18-12-10-14)8-7-15-6-5-13-3-1-2-4-16(13)19-15/h1-12H/b8-7+
InChi Key
UJJUKZPBUMCSJZ-BQYQJAHWSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $49

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    10 mg

    $83

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    25 mg

    $182

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    50 mg

    $291

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    Product Description

    6-Phosphofructo-2-kinase/fructose-2,6-bisphosphatase 3 (PFKFB3) is a bifunctional enzyme that contains distinct domains for the phosphorylation of fructose 6-phosphate and the dephosphorylation of fructose 2,6-bisphosphate. PFKFB3 protein expression is elevated in most tumor types.1,2 PFK15 is a selective inhibitor of PFKFB3 (IC50 = 207 nM).3 It has no significant inhibitory effect on any member of a panel of 96 other kinases, and does not inhibit purified 6-phosphofructo-1-kinase, hexokinase, phosphoglucose isomerase, or PFKFB4. PFK15 rapidly induces apoptosis in transformed cells, suppresses glucose uptake and growth of Lewis lung carcinomas in syngeneic mice, and yields antitumor effects in human xenograft models of cancer in athymic mice.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Atsumi, T., Chesney, J., Metz, C., et al. High expression of inducible 6-phosphofructo-2-kinase/fructose-2,6-bisphosphatase (iPFK-2; PFKFB3) in human cancers. Cancer Res. 62(20), 5881-5887 (2002).

    2. Seo, M., Kim, J.D., Neau, D., et al. Structure-based development of small molecule PFKFB3 inhibitors: A framework for potential cancer therapeutic agents targeting the Warburg effect. PLoS One 6(9), e24179 (2011).

    3. Clem, B.F., O'Neal, J., Tapolsky, G., et al. Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer. Mol. Cancer Ther. 12(8), 1461-1470 (2013).