Hydrolases (Ether)
Soluble expoxide hydrolase (sEH; EC 3.3.2.10) is a key enzyme in the metabolism of eicosanoid epoxides, including epoxyeicosatrienoic acids (EETs) and of leukotoxin (LTX). EETs, endothelium-derived hyperpolarizing factors, exhibit potentially beneficial properties, including anti-inflammatory effects and vasodilation. The enzyme is a bifunctional homodimeric complex located in both cytosol and peroxisomes with hydrolase and phosphatase activity[1]. GSK2256294A (Axon 2220) is a potent, selective inhibitor of sEH, and attenuates cigarette smoke-induced inflammation by both inhibiting its initiation and/or maintenance and promoting its resolution. GSK2256294A would be an appropriate agent to evaluate the role of sEH in clinical studies, for example in diseases where cigarette smoke is a risk factor, such as chronic obstructive pulmonary disease (COPD) and cardiovascular disease[2].
[1] H.C. Shen. Soluble epoxide hydrolase inhibitors: a patent review. Expert Opin. Ther. Pat. 2010, 20, 941-956.
[2] P.L. Podolin et al. In vitro and in vivo characterization of a novel soluble epoxide hydrolase inhibitor. Prostaglandins Other Lipid. Mediat. 2013, 104-105, 25-31.
| Axon ID | Name | Description | From price | |
|---|---|---|---|---|
| 3022 | TUPS | Soluble epoxide hydrolase inhibitor | €135.00 | |
| 2220 | GSK 2256294A | Potent, reversible, tight binding inhibitor of recombinant human sEH | €125.00 | |
| 2307 | ARM1 hydrobromide | Novel type of LTA4H inhibitor that selectively blocks the conversion of LTA4 into LTB4 | €92.00 | |