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Cathepsin G Inhibitor I

In stock
Catalog No.
A8174
Cathepsin G inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$360.00
In stock
Evaluation Sample
$28.00
In stock
1mg
$80.00
In stock
5mg
$160.00
In stock
10mg
$250.00
In stock

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Email: [email protected]

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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.

Reference:
[1] 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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt620.64
Cas No.429676-93-7
FormulaC36H33N2O6P
Solubility≥10.35mg/mL in DMSO
Chemical Name[2-[3-[(1-benzoylpiperidin-4-yl)-methylcarbamoyl]naphthalen-2-yl]-1-naphthalen-1-yl-2-oxoethyl]phosphonic acid
SDFDownload SDF
Canonical SMILESCN(C1CCN(CC1)C(=O)C2=CC=CC=C2)C(=O)C3=CC4=CC=CC=C4C=C3C(=O)C(C5=CC=CC6=CC=CC=C65)P(=O)(O)O
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Cathepsin G Inhibitor I is a potent, selective, reversible, competitive, non-peptide inhibitor of cathepsin G.
Targets cathepsins G          
IC50 53nM          

Quality Control

Quality Control & MSDS

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Chemical structure

Cathepsin G Inhibitor I