VU0155069

Non disponible en dehors du Royaume-Uni et de l'Irlande

Biochem/physiol Actions

VU0155069 is a PLD1-selective catalytic site-targeting phospholipase D inhibitor (PLD1/2 IC50 = 46 nM/933 nM by cell-free enzymatic assays; substrate = di-palmitoyl-PLC) that selectively suppresses the cellular PLD activity in PMA-stimulated non-small-cell lung cancer (NSCLC) Calu-1 cells with predominant PLD1 activity over GFP-PLD2-overexpressing HEK293 cells (IC50 = 11 nM and 1.8 µM, respectively). Note: VU0155069 is reported to impair P2X7-induced pore formation in human RPMI 8226 B cells lacking PLD1 expression.