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Overview
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Background
IC50: 53 nM Cathepsin G (EC 3.4.21.20, chymotrypsin-like proteinase, neutral proteinase) is an enzymatic protein belonging to the peptidase or protease families. In humans, it is coded by the CTSG gene. Cathepsin G Inhibitor I is a potent, selective, reversible, competitive, non-peptide inhibitor of cathepsin G. In vitro: Cathepsin G Inhibitor I shows reversible, competitive inhibition with IC50 and Ki values of 53 ± 12 (N = 10) and 63 ± 14 nM (N = 5), respectively. Another attribute of Cathepsin G Inhibitor I relates to its selectivity vs other serine proteases. It weakly inhibits chymotrypsin (Ki = 1.5 ± 0.2 μM), and poorly inhibits (<50% inhibition at 100 μM) thrombin, factor Xa, factor IXa, plasmin, trypsin, tryptase, proteinase 3, and human leukocyte elastase [1]. In vivo: Cathepsin G Inhibitor I is currently in in-vitro investigation and no animal in vivo study is ongoing [1]. Clinical trial: Cathepsin G Inhibitor I is currently in the preclinical development and no clinical trial is ongoing.
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Overview