Catalog No.S7289 Synonyms: PFK-015
Molecular Weight(MW): 260.29
PFK15 is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.
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RA FLSs were pretreated with DMSO (as the control) or various concentrations of a specific PFKFB3 inhibitor, PFK15, for 4 h (A). The expression of IL-6, IL-8, CCL-2 and CXCL-10 was measured by real-time qPCR. The data are representative of independent experiments (means ± SEM) from10 RA patients. *P < 0.05, significantly different from control or SiC; #P < 0.05, significantly different from treatment with TNF-α alone
Br J Pharmacol, 2017, 174(9):893-908. PFK15 purchased from Selleck.
(a, b) Cells were treated with the indicated concentrations of PFK15 for 12 h in the upper chambers and the lower chambers were filled with 10% FBS medium. Then, the invaded cells were stained with crystal violet and observed under a microscope with 200× magnification. Data were obtained from six randomly chosen fields and were normalized to the control group. (c) Proteins related with cell migration and invasion were detected. Phospho-FAK levels were downregulated in 7 and 9 μM while phospho-Cadherin E levels upregulated in both cell lines. Columns, mean; bars, SD. *P<0.05, compared with controls.
PLoS One, 2016, 11(9):e0163768. PFK15 purchased from Selleck.
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|Description||PFK15 is a potent and selective 6-phosphofructo-2-kinase (PFKFB3) inhibitor with IC50 of 207 nM.|
PFK15 produces potent growth inhibition in a series of cancer cells. In Jurkat T-cell leukemia cells and H522 lung adenocarcinoma cells, PFK15 also reduces F26BP, glucose uptake, and intracellular ATP level. 
|In vivo||In vivo, PFK15 has adequate pharmacokinetic properties. PFK15 (25 mg/kg i.p.) suppresses the growth, metastatic spread, and glucose metabolism of LLC tumors in syngeneic mice. In three human xenograft models of cancer in athymic mice, PFK15 also yields antitumor effects that are comparable to approved chemotherapeutic agents. |
Recombinant PFKFB3 assay:Kinase reactions are conducted by incubating 13 ng of recombinant human PFKFB3 protein in a reaction mix containing 10 μmol/L ATP, 10 μmol/L F6P, and either dimethyl sulfoxide (DMSO) vehicle control, 3PO, or PFK15 for 1 hour at room temperature. Kinase activity is measured with the Adapta Universal Kinase Assay per manufacturer
|In vitro||DMSO||19 mg/mL warmed (72.99 mM)|
|Ethanol||2 mg/mL warmed (7.68 mM)|
|In vivo||Add solvents individually and in order:
5% DMSO+45% PEG 300+1% Tween 80+ddH2O
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
C17 H12 N2 O
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
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