Cathepsin C Inhibitor

E 64c is a derivative of naturally occurring epoxide inhibitor of cysteine proteases, a Calcium-activated neutral protease (CANP) inhibitor and a very weak irreversible cathepsin C inhibitor. E 64c exhibits entry-blocking effect for MERS-CoV.

GSK-2793660 is an orally active and irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 can be used for the research of bronchiectasis.

GSK-2793660 (free base) is an oral, irreversible inhibitor of Cathepsin C (CTSC). GSK-2793660 (free base) can be used for the research of bronchiectasis.

Z-Val-Val-Nle-diazomethylketone is a cathepsin S (CATS) inhibitor. Z-Val-Val-Nle-diazomethylketone significantly inhibits the IFNg-induced upregulation of the MHCII molecules HLA-DR and Ii-p33/35 with an increase of Ii-p10 protein level. Z-Val-Val-Nle-diazomethylketone can be used for dermatological diseases like psoriasis, atopic dermatitis and actinic keratosis research.

Cathepsin C-IN-4 (compound SF27) is a potent Cathepsin C (Cat C) inhibitor, with an IC₅₀ of 65.6 nM. Cathepsin C-IN-4 also inhibits THP-1 and U937 cell, with IC₅₀ values of 203.4 and 177.6 nM, respectively.

Cathepsin L-IN-6 (Compound 6a) is a selective cathepsin L inhibitor with an IC₅₀ of 0.021 μM. Cathepsin L-IN-6 suppresses cathepsin L activity by directly binding to cathepsin L. Cathepsin L-IN-6 inhibits IL-6 and IL-8. Cathepsin L-IN-6 shows a high anti-inflammatory activity. Cathepsin L-IN-6 can be used in the research of acute lung injury.

Cathepsin C-IN-3 (compound SF11) is a potent Cathepsin C (Cat C) inhibitor, with an IC₅₀ of 61.79 nM. Cathepsin C-IN-3 also inhibits THP-1 and U937 cell, with IC₅₀ values of 101.5 and 86.5 nM, respectively.

Cathepsin C-IN-7 (Page 68) is a Cathepsin C inhibitor. Cathepsin C-IN-7 can be used in research related to primary cancers and cancer metastases.

BI-9740 is an orally active and selective cathepsin C (CatC) inhibitor, with an IC₅₀ of 0.6 nM in mice and 2.6 nM in rats. BI-9740 can inhibit the production of active neutrophil elastase. Additionally, BI-9740 is capable of reducing the activities of neutrophil elastase and cathepsin G in the bone marrow of rats, alleviating pathological damage to grafts after heart transplantation, shortening the reperfusion time, and improving left ventricular function. BI-9740 can be used in research related to organ transplantation.

Verducatib (BI 1291583) is an orally active inhibitor of cathepsin C (also known as DPP1). Verducatib restores the protease-inhibitor balance by inhibiting the activation of neutrophil serine proteases, thereby alleviating pulmonary inflammation and regulating infection responses. Verducatib significantly reduces the risk (including severe exacerbations) and frequency of acute exacerbations in bronchiectasis (BE). Verducatib also improves lung function and quality of life, and shortens the duration of antibiotic use. The overall incidence of adverse events of Verducatib is comparable to that of placebo, with only slightly more mild-to-moderate cutaneous adverse events observed in the high-dose group, demonstrating promising clinical application potential.

AM4299 A is a thiol protease inhibitor with IC₅₀ values of 73, 390 and 88 nM against Cathepsin B, Cathepsin L and Papain, respectively. AM4299 A shows low toxicity and favorable biosafety in mice. AM4299 A can be used in studies related to osteoporosis and parasitic diseases.