PFK-015

Short Summary : PFKFB3 inhibitor, potent and selective

Category :

Purity : 0.98

CAS Number : 4382-63-2

Formula : C17H12N2O

Molecular Weight :

Molecular Weight : 260.29

SMILE : O=C(C1=CC=NC=C1)/C([H])=C([H])/C2=NC3=CC=CC=C3C=C2

Solubility : >13mg/mL in DMSO

Storage : Store at -20°C

Description : PFK-015 is a potent and selective inhibitor of PFKFB3 with IC50 value of 207 nM [1].
6-phosphofructo-2-kinase (PFKFB3) is an enzyme that is encoded by the PFKFB3 gene in humans. PFKFB3 is a direct transcriptional target of HIF- and is activated by oncogenic AKT and Ras and stabilized by the loss of the tumor suppressor PTEN via suppressive effects on APC/Cdh1-mediated ubiquitination [1].
PFK-015 is a potent and selective PFKFB3 inhibitor. In H522 lung adenocarcinoma and Jurkat cell lines, PFK15 exhibited cytotoxic effects with IC50 values of 2.42 and 0.72 M in Jurkat and H522, respectively. Also, PFK15 reduced glucose uptake, intracellular ATP and F26BP, the substrate of PFKFB3. In Jurkat T cell leukemia cells, PFK15 (3 M) increased the number of cells undergoing early apoptosis. PFK15 (3 and 20 M) increased the number of cells undergoing late apoptosis in a dose dependent way [1].
In Lewis lung carcinoma (LLC)-bearing mice, PFK15 inhibited LLC cells metastasized from the subcutaneous to the lungs. PFK15 decreased tumor-associated F26BP and significantly increased the number of cells that were positive for cleaved caspase 3. Also, PFK15 reduced fluoro-D-glucose (18F-FDG) uptake by 50%. PFK15 inhibited the growth of colon and pancreatic adenocarcinomas [1].
Reference:[1]. Clem BF, O’Neal J, Tapolsky G, et al. Targeting 6-phosphofructo-2-kinase (PFKFB3) as a therapeutic strategy against cancer. Mol Cancer Ther, 2013, 12(8): 1461-1470.

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