CAY10594

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. CAY10594 is a potent PLD₂ inhibitor, both in vitro (IC₅₀ = 140 nM) and in cells (IC₅₀ = 110 nM).¹ It is also effective as a PLD₁ inhibitor at higher concentrations (IC₅₀ = 5.1 μM in vitro, 1.0 μM in cells).¹ CAY10594 strongly inhibits the invasive migration of breast cancer cells 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).

Leis, H.J., and Windischhofer, W. Phospholipase D₁ activity is crucial for cytosolic phospholipase A₂ -dependent prostaglandin E₂ formation in murine osteoblastic MC3T3-E₁ cells. Prostaglandins Leukot. Essent. Fatty Acids 198-199, 102592 (2023).