PHOP

PHOP is a potent FAAH inhibitor, exhibiting K_i values of 0.094 nM and 0.2 nM for the human and rat enzymes, respectively.¹ Using a proteomics approach, PHOP was screened against the serine hydrolase family of enzymes, of which FAAH is a member. In this assay, PHOP exhibited IC₅₀ values of 1.1 nM, 1.4 nM, and >100 µM for FAAH, triacylglycerol hydrolase (TGH), and an uncharacterized hydrolase (KIAA1363), respectively.² Knowledge of the specificity of PHOP obtained from this experiment should allow for more accurate interpretation of results using this inhibitor in complex environments such as whole cells or animals.

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1. Boger, D.L., Sato, H., Lerner, A.E., et al. Exceptionally potent inhibitors of fatty acid amide hydrolase: The enzyme responsible for degradation of endogenous oleamide and anandamide. Proc. Natl. Acad. Sci. USA 97(10), 5044-5049 (2000).

2. Leung, D., Hardouin, C., Boger, D.L., et al. Discovering potent and selective reversible inhibitors of enzymes in complex proteomes. Nat. Biotechnol. 21(6), 687-691 (2003).