Cayman R-59-022

Diacylglycerol (DAG) kinases (DGKs) phosphorylate DAG to give phosphatidic acid (PA), reducing signaling through DAG and increasing signaling through PA.¹ R-59-022 is an inhibitor of DGK (IC₅₀ = 2.8 µM).² This results in increased DAG-dependent PKC activity and potentiates aggregation of thrombin-stimulated platelets.^2,3 R-59-022 also blocks vascular contraction induced by the thromboxane analog U-46619 (Item No. 16450).⁴ At 10 µM, R-59-022 induces apoptosis in glioblastoma cells without being toxic to non-cancerous cells.⁵ It inhibits DGK-θ in vitro at concentrations below 1 µM and blocks DGK-θ activity in vivo.⁶ R-59-022 also inhibits A. thaliana DGK2 (IC₅₀ = 50 µM) and suppresses root growth but does not affect DGK7 at 50 µM.⁷

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