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Beschreibung

A cell-permeable, 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. It 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. Unlike 1-butanol, this compound does not affect glucose-stimulated insulin secretion in Min6 pancreatic beta-cells.