VU0155069

Phospholipase D (PLD) is an enzyme which cleaves the head group from phospholipids, producing the second messenger phosphatidic acid. Two mammalian isoforms of PLD, PLD1 and PLD2, have been identified, with multiple splice variants of each. Although the two isoforms share structural and functional features, they are regulated differently and apparently subserve distinct roles. VU0155069 is a potent and selective inhibitor of phospholipase D (PLD)1, both in vitro (IC50 = 46 nM) and in cells (IC50 = 11 nM).{16821} It is also effective as a PLD2 inhibitor at higher concentrations (IC50 = 933 nM in vitro; 1,800 nM in cells).{16821} VU0155069 strongly inhibits the invasive migration of several breast cancer cell lines in transwell assays, suggesting that PLD might be a useful target in blocking tumor cell invasion.{16821}