A cathepsin G inhibitor
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Cathepsin G Inhibitor I

Item No. 14928

Technical Information
Formal Name
P-[2-[3-[[(1-benzoyl-4-piperidinyl)methylamino]carbonyl]-2-naphthalenyl]-1-(1-naphthalenyl)-2-oxoethyl]-phosphonic acid
CAS Number
429676-93-7
Molecular Formula
C36H33N2O6P
Formula Weight
Purity
≥95%
Formulation
A crystalline solid
DMF: 5 mg/mlDMSO: 10 mg/mlDMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml
λmax
224, 248 nm
SMILES
O=C(N(C1CCN(C(C2=CC=CC=C2)=O)CC1)C)C3=CC4=CC=CC=C4C=C3C(C(C5=CC=CC6=C5C=CC=C6)P(O)(O)=O)=O
InChi Code
InChI=1S/C36H33N2O6P/c1-37(28-18-20-38(21-19-28)35(40)25-11-3-2-4-12-25)36(41)32-23-27-14-6-5-13-26(27)22-31(32)33(39)34(45(42,43)44)30-17-9-15-24-10-7-8-16-29(24)30/h2-17,22-23,28,34H,18-21H2,1H3,(H2,42,43,44)
InChi Key
GNOZQRKYZJSIPZ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    Cathepsin G inhibitor I is an inhibitor of cathepsin G (IC50 = 53 nM).1 It is selective for cathepsin G over various serine proteases, including thrombin, Factor Xa, Factor IXa, plasmin, trypsin, and leukocyte proteinase 3 (PR3; IC50s = >100 µM for all), but also weakly inhibits chymotrypsin. It inhibits cathepsin G-induced activation of IL-36 in neutrophil degranulates when used at a concentration of 10 µM.2 Cathepsin G inhibitor I (10 µM) reduces CD4+ T cell-induced secretion of IFN-γ and IL-17 in B cells incubated with tetanus toxin C-fragments (TTC) and also reduces TTC presentation in B cells.3 It decreases the size of neuromyelitis optica lesions and reduces the number of perivascular neutrophils, indicating decreased neutrophil brain entry, when used in combination with the neutrophil elastase inhibitor sivelestat (Item No. 17779) in a mouse model of IgG-induced brain injury when administered intracerebrally at a dose of 5 µg/animal.4

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Greco, M.N., Hawkins, M.J., Powell, E.T., et alNonpeptide inhibitors of cathepsin G: Optimization of a novel β-ketophosphonic acid lead by structure-based drug design. J. Am. Chem. Soc. 124(15), 3810-3811 (2002).

    2. Henry, C.M., Sullivan, G.P., Clancy, D.M., et alNeutrophil-derived proteases escalate inflammation through Aactivation of IL-36 family cytokines. Cell Rep. 14(4), 708-722 (2016).

    3. Reich, M., Lesner, A., Legowska, A., et alApplication of specific cell permeable cathepsin G inhibitors resulted in reduced antigen processing in primary dendritic cells. Mol. Immunol. 46(15), 2994-2999 (2009).

    4. Saadoun, S., Waters, P., MacDonald, C., et alNeutrophil protease inhibition reduces neuromyelitis optica-immunoglobulin G-induced damage in mouse brain. Ann. Neurol. 71(3), 323-333 (2012).

    Product Citations

    Xiao, Y., Cong, M., Li, J., et alCathepsin C promotes breast cancer lung metastasis by modulating neutrophil infiltration and neutrophil extracellular trap formation. Cancer Cell 39(3), 423-437 (2021).