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).¹ It is also effective as a PLD₂ inhibitor at higher concentrations (IC₅₀ = 933 nM in vitro; 1,800 nM in cells).¹ 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.¹

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1. Scott, S.A., Selvy, P.E., Buck, J.R., et al. Design of isoform-selective phospholipase D inhibitors that modulate cancer cell invasiveness. Nat. Chem. Biol. 5(2), 108-117 (2009).