Cathepsin G Inhibitor I
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.
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 620.64 |
| Cas No. | 429676-93-7 |
| Formula | C36H33N2O6P |
| Solubility | ≥10.35 mg/mL in DMSO |
| Chemical Name | [2-[3-[(1-benzoylpiperidin-4-yl)-methylcarbamoyl]naphthalen-2-yl]-1-naphthalen-1-yl-2-oxoethyl]phosphonic acid |
| SDF | Download SDF |
| Canonical SMILES | CN(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 Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
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Cell lines |
Metastatic breast cancer cells and neutrophils |
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Reaction Conditions |
2 μM cathepsin G inhibitor I for 22 h incubation |
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Applications |
Cathepsin G inhibitor I (2 μM) reduced the formation of neutrophil extracellular traps (NETs) induced by cancer cells. In addition, cathepsin G inhibitor I (2 μM) inhibited neutrophil-stimulated invasion. Thus, inhibition of cathepsin G, a protease associated with NETs, was able to reduce the extension of NETs and block neutrophils’ ability to promote invasion. |
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Note |
The technical data provided above is for reference only. |
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References: 1. Park J, Wysocki RW, Amoozgar Z, et al. Cancer cells induce metastasis-supporting neutrophil extracellular DNA traps. Science Translational Medicine, 2016, 8(361): 361ra138. |
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| Cathepsin G Inhibitor I is a potent, selective, reversible, competitive, non-peptide inhibitor of cathepsin G. | ||||||
| Targets | cathepsins G | |||||
| IC50 | 53nM | |||||
Quality Control & MSDS
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Chemical structure
