PFK-015 (PFK15) is an effective inhibitor of PFKFB3 (IC50: 110 nM) and inhibits PFKFB3 activity in Y cells (IC50: 20 nM).

PFKFB3:110 nM, PFKFB3:20 nM

PFK-015（25 mg/kg,i.p.）对同源小鼠体内LLC肿瘤的生长、转移扩散及葡萄糖代谢具有抑制作用.在三个人异种移植的无胸腺癌症小鼠模型中,PFK-015与公认化疗药物的抗癌效果相似.PFK-015有适当的体内药代动力学性质.

在Jurkat T-细胞白血病细胞和H522肺腺癌细胞中,PFK-015可使F26BP、葡萄糖摄取及细胞内腺嘌呤核苷三磷酸水平降低。PFK-015还对一系列癌细胞的生长具有明显的抑制作用。

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

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)