SC-39026, a specific human neutrophil elastase inhibitor |
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Authors: | A Nakao R A Partis G P Jung R A Mueller |
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Affiliation: | 1. Department of Biochemistry, University of Zurich, CH-8057, Zurich, Switzerland;2. Koch Institute for Integrative Cancer Research, Massachusetts Institute of Technology, Cambridge, MA 02139, USA;3. Department of Chemistry and Applied Biosciences, ETH Zurich, CH-8093, Zurich, Switzerland |
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Abstract: | SC-39026, (+/-) 2-chloro-4-(1-hydroxyoctadecyl)benzoic acid, inhibits human neutrophil elastase with an IC50 of 0.5 microM (KI of 1.5 microM). Its inhibition of elastase is reversible and noncompetitive at low concentrations (0.5-1.25 microM). Inhibition is "mixed" at higher inhibitor concentrations. SC-39026 is inactive against hog pancreatic elastase, bovine alpha-chymotrypsin and Pseudomonas aeruginosa elastase, but does inhibit human neutrophil cathepsin G with an IC50 of approximately 2.5 microM. Neutrophil elastases isolated from rat, hamster, rabbit and hog are also inhibited by SC-39026. |
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