FIPI is a cell-permeable, PC-PLD1/2 (PLD1/2) inhibitor (IC50 = 1 nM and 10 nM for PLD1 and PLD2, respectively, in a CHO cell based assay, and IC50 = 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.
1 Su, W., Yeku, O., Olepu, S., et al. 5-fluoro-2-indolyl des-chlorohalopemide (FIPI), a phospholipase D pharmacological inhibitor that alters cell spreading and inhibits chemotaxis. Mol Pharmacol 75(3) 437-446 (2009). 2 Monovich, L., Mugrage, B., Quadros, E., et al. Optimization of halopemide for phospholipase D2 inhibition. Bioorg Med Chem Lett 17 2310-2311 (2007).
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