| Name | PFK-015 |
| Description | PFK-015 (PFK15) is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM). |
| Cell Research | Viability is determined using trypan blue exclusion. Cells were incubated in 20% trypan blue for 5 minutes. Cells excluding trypan blue are counted using a standard hemocytometer to determine the total number of viable cells. Experiments are conducted in triplicate. (Only for Reference) |
| Kinase Assay | 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 | PFK-015 (25 mg/kg, i.p.) inhibits the growth, metastatic spread, and glucose metabolism of LLC tumors in syngeneic mice. In three distinct athymic mouse models of xenografted human cancers, the anticancer efficacy of PFK-015 is comparable to that of established chemotherapy drugs. PFK-015 exhibits favorable pharmacokinetic properties in vivo. |
| In vivo | PFK-015 effectively reduces levels of F26BP, glucose uptake, and intracellular adenosine triphosphate (ATP) in Jurkat T-cell leukemia cells and H522 lung adenocarcinoma cells. Additionally, PFK-015 exhibits significant inhibitory effects on the growth of a variety of cancer cells. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 3 mg/mL (11.53 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (3.84 mM), Sonication is recommended.
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| Keywords | stomach cancer | PFKFB3 | PFK-15 | PFK-015 | PFK015 | PFK 15 | lung cancer | Inhibitor | inhibit | esophageal squamous cell carcinoma (ESCC) | colon cancer | cancers | Autophagy | 3PO |
| Inhibitors Related | Stavudine | Aceglutamide | Hemin | Tamoxifen | Cysteamine hydrochloride | Guanidine hydrochloride | Hydroxychloroquine | Enzalutamide | Paeonol | Naringin | Alginic acid | Sildenafil citrate |
| Related Compound Libraries | Glycometabolism Compound Library | Glycolysis Compound Library | Bioactive Compound Library | ReFRAME Related Library | Kinase Inhibitor Library | Autophagy Compound Library | Inhibitor Library | NO PAINS Compound Library | Metabolism Compound Library | Anti-Aging Compound Library | Bioactive Compounds Library Max | Anti-Metabolism Disease Compound Library |
United States
