名称 | PFK-015 |
描述 | PFK-015 (PFK15) is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM). |
细胞实验 | 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) |
激酶实验 | 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 |
体外活性 | 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. |
体内活性 | 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. |
存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
溶解度 | DMSO : 3 mg/mL (11.53 mM), Sonication is recommended.
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关键字 | Autophagy | PFK-15 | 3PO | stomach cancer | cancers | inhibit | PFK 15 | PFKFB3 | esophageal squamous cell carcinoma (ESCC) | PFK015 | lung cancer | colon cancer | Inhibitor | PFK-015 |
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相关库 | 糖酵解化合物库 | 表型筛选靶点鉴定库 | 经典已知活性库 | 激酶抑制剂库 | 抗癌细胞代谢库 | 抑制剂库 | NO PAINS 化合物库 | 代谢化合物库 | 抗衰老化合物库 | 已知活性化合物库 |