|Cathepsin G Inhibitor ICathepsin G inhibitor|
Sample solution is provided at 25 µL, 10mM.
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|Cathepsin G Inhibitor I is a potent, selective, reversible, competitive, non-peptide inhibitor of cathepsin G.|
|Cas No.||429676-93-7||SDF||Download SDF|
|Chemical Name||[2-[3-[(1-benzoylpiperidin-4-yl)-methylcarbamoyl]naphthalen-2-yl]-1-naphthalen-1-yl-2-oxoethyl]phosphonic acid|
|Solubility||>10.4mg/mL in DMSO||Storage||Store at -20°C|
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IC50: 53 nM
Cathepsin G (EC 126.96.36.199, 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 .
In vivo: Cathepsin G Inhibitor I is currently in in-vitro investigation and no animal in vivo study is ongoing .
Clinical trial: Cathepsin G Inhibitor I is currently in the preclinical development and no clinical trial is ongoing.
 Greco MN, Hawkins MJ, Powell ET, Almond HR Jr, Corcoran TW, de Garavilla L, Kauffman JA, Recacha R, Chattopadhyay D, Andrade-Gordon P, Maryanoff BE. Nonpeptide inhibitors of cathepsin G: optimization of a novel beta-ketophosphonic acid lead by structure-based drug design. J Am Chem Soc. 2002;124(15):3810-1.