Fatty acid amide hydrolase (FAAH) is the enzyme responsible for hydrolysis and inactivation of fatty acid amides including anandamide and oleamide. CAY10435 is a selective, potent inhibitor of rat FAAH exhibiting a Ki value of 0.57 nM. Using a proteonomics approach, CAY10435 was screened against the serine hydrolase family of enzymes, of which FAAH is a member. In this assay, CAY10435 exhibited IC50 values of 0.81 nM, 83 nM, and 50 μM for FAAH, triacylglycerol hydrolase (TGH), and an uncharacterized hydrolase (KIAA1363), respectively. Knowledge of the specificity of CAY10435 obtained from this experiment should allow for more accurate interpretation of results using the inhibitor in complex environments such as whole cells or animals.
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