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Inhibition of recombinant DAGLα and β by 39 and 40. Inhibitory activity of the alkyne (A) and biotin (B) probes, 39 and 40, respectively, was measured by competitive ABPP using DAGL-HEK293T membrane lysates. Proteomes were preincubated with varying concentrations of 39 or 40 for 30 min at 37 °C prior to treatment with 38 (1 μM, 30 min, 37 °C) and analysis by gel-based ABPP. Both probes blocked 38 labeling of DAGLα and β with IC50 values ranging from 0.4 – 2 μM.
