A cell-permeable, PLD1/2 inhibitor (IC50=1nM and 10nM for PLD1 and PLD2, respectively, in a CHO cell based assay, and IC50=20nM 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 750nM. Unlike 1-butanol, this compound does not affect glucose-stimulated insulin secretion in Min6 pancreatic b-cells.
Synonyms:Compound 4k, PLD Inhibitor I
Molecular Formula:C₂₃H₂₄FN₅O₂
Molecular Weight:421.2
Solubility:DMSO (100mg/ml)
Storage and Stability:Store at -20°C under inert atmosphere. Protect from light. For maximum recovery of product, centrifuge the original vial prior to removing the cap.
