compound introduction
FIPI是一种可透过细胞的PC-PLD1 / 2（PLD1 / 2）抑制剂（在基于CHO细胞的测定中，PLD1和PLD2的IC | 50 | = 1 nM和10 nM，IC | 50 | = 20在生化分析中，PLD2的浓度为nM），对MitoPLD无活性，并且对PLD1和PLD2的选择性高于其他PLD超家族酶。还显示FIPI可以阻止CHO细胞中细胞骨架重组和细胞运输的PLD2依赖性作用，并在750 nM时减少HL60细胞中由fMLP定向的嗜中性粒细胞趋化性。 FIPI is a cell-permeable, PC-PLD1/2 (PLD1/2) inhibitor (IC|50|= 1 nM and 10 nM for PLD1 and PLD2, respectively, in a CHO cell based assay, and IC|50|= 20 nM for PLD2 in a biochemical assay), that displays no activity toward MitoPLD, and is selective for PLD1 and PLD2 over other PLD superfamily enzymes. FIPI is also shown to block PLD2-dependent effects on cytoskeletal reorganization and cell trafficking in CHO cells, and diminish fMLP-directed neutrophil chemotaxis in HL60 cells at 750 nM.
