Phenyl hexanoyl oxazolopyridine (PHOP) is a potent FAAH inhibitor (K|i|= 0.094 nM and 0.2 nM for the human and rat enzymes, respectively). 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 IC|50|values of 1.1 nM, 1.4 nM, and >100 μM for FAAH, triacylglycerol hydrolase (TGH), and an uncharacterized hydrolase (KIAA1363), respectively. 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.
1.Wang Yue, Xiao Han, Yang Lei, Jia Xiaojing, Guo Xuan, Zhang Zhaobin. (2020) In vivo estrogenicity of p-phenoxyphenol and p-pentyloxyphenol. Scientific Reports, 10 (1):(1-11). [PMID:33057140][10.1038/s41598-020-73271-1]
References
1.Wang Yue, Xiao Han, Yang Lei, Jia Xiaojing, Guo Xuan, Zhang Zhaobin. (2020) In vivo estrogenicity of p-phenoxyphenol and p-pentyloxyphenol. Scientific Reports, 10 (1):(1-11). [PMID:33057140][10.1038/s41598-020-73271-1]
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