Search by product name, CAS, target or catalog number. Press Down Arrow to reach product suggestions, Tab to move between links, and Escape to close suggestions.
Cathepsin inhibitors act on lysosomal proteases, mainly the papain-like cysteine cathepsins B, C, K, L and S. Cysteine cathepsins degrade proteins in the endolysosomal system and, after secretion, also remodel the extracellular matrix. In 1996 loss of cathepsin K was shown to cause pycnodysostosis, a lysosomal disease with dense, brittle bones. Cathepsin K is the main collagen-degrading protease of osteoclasts, which makes it a target in bone resorption studies. Odanacatib and balicatib inhibit cathepsin K, petesicatib targets cathepsin S, and CA-074 is selective for cathepsin B. CA-074 methyl ester is a membrane-permeable form for work in intact cells. Gly-Phe-beta-naphthylamide, a cathepsin C substrate, is used to rupture lysosomes in live cells.
Dutacatib is a selective inhibitor of cathepsin K with demonstrated antiviral activity against SARS-CoV-2 3CLpro. By inhibiting cathepsin K, it plays a role in ameliorating bone diseases associated with cancer. This compound is valuable for research focused on therapeutic interventions in viral infections and bone-related pathologies in cancer.
SQ 32602 is a potent inhibitor of cathepsin E, exhibiting an IC50 value of 88 nM. This compound selectively inhibits cathepsin E activity, making it valuable for research into lysosomal function and proteolytic processes. SQ 32602 is suitable for studies involving cancer biology, autoimmune diseases, and other conditions where cathepsin E modulation may play a critical role.
Out of stock
All 3 sizes
Synonyms: VEL 0230
NC 2300 is a selective and orally active inhibitor of cysteine cathepsins, specifically targeting cathepsin B, K, and S with IC50 values of 284, 34.5, and 186 nM, respectively. This compound is particularly useful in the study of diseases related to bone mineral disorders, enabling researchers to explore the role of cathepsins in these conditions and potential therapeutic interventions.
TB-11 is a potent Cathepsin D inhibitor, demonstrating an IC50 of 0.126 nM for Cathepsin D, alongside inhibitory activity of 1.92 nM for Cathepsin E and 48.8 nM for BACE1. This compound is valuable for research focused on tumor biology and the role of cathepsins in cancer progression. Its selectivity and potency make it a useful tool for investigating the therapeutic potential of Cathepsin D inhibition in various oncological studies.
Out of stock
All 3 sizes
Cathepsin K-IN-9 is a potent and selective inhibitor of Cathepsin K, exhibiting an IC50 of 6.2 nM. It demonstrates remarkable selectivity with IC50 values exceeding 10,000 nM for Cathepsins B, L, and S, providing over 1600-fold selectivity. With its excellent safety profile and metabolic stability, Cathepsin K-IN-9 is suitable for research applications in osteoporosis and other bone resorption-related studies.
Out of stock
All 3 sizes
Synonyms: TG0205221
MPI8 is an inhibitor of the major protease of SARS-CoV-2 (MPro) and cathepsin L, exhibiting significant antiviral activity. It functions through dual and selective inhibition of these key proteases, impacting the viral life cycle and host cellular processes. MPI8 is suitable for use in clinical studies targeting COVID-19 and contributes to understanding therapeutic strategies against SARS-CoV-2.
BML-244 is a potent inhibitor of cathepsin K, a cysteine proteinase involved in various pathological processes. This compound demonstrates significant biological activity in the context of inflammatory conditions, making it valuable for research applications related to rheumatoid arthritis (RA) and periodontitis. The inhibition of cathepsin K by BML-244 facilitates the exploration of its role in bone resorption and tissue remodeling, contributing to a better understanding of these diseases.
Cathepsin S-IN-1 is a potent inhibitor of Cathepsin S, a cysteine protease involved in the regulation of immune responses and antigen processing. By selectively targeting Cathepsin S, this compound can modulate inflammatory pathways and contribute to studies on autoimmune diseases, cancer, and other pathological conditions linked to protease activity. Its application in research may provide insights into therapeutic strategies aimed at inhibiting Cathepsin S-mediated processes.
MDL 27399 is a selective inhibitor of human neutrophil cathepsin G, exhibiting a Ki value of 7 μM. This compound is instrumental in studying the role of cathepsin G in inflammatory diseases, allowing researchers to explore potential therapeutic avenues for conditions characterized by excessive neutrophil activity.
Verducatib is an orally active inhibitor of cathepsin C, also known as Dipeptidyl Peptidase I (DPP1). By inhibiting the activation of neutrophil serine proteases, Verducatib restores the balance of proteases and inhibitors, thereby reducing pulmonary inflammation and enhancing responses to infection. This compound has demonstrated efficacy in decreasing the frequency and severity of acute exacerbations in bronchiectasis, while also improving lung function and quality of life. Its safety profile is comparable to placebo, with a slight increase in mild-to-moderate cutaneous adverse events at higher doses, indicating potential for clinical application.
Gallinamide A is a potent inhibitor of cathepsin L, demonstrating an IC50 value of 17.6 pM. This compound plays a crucial role in research applications focused on investigating the functions of cathepsin L in various biological processes, including protein degradation and immune response regulation. Its inhibitory activity makes Gallinamide A a valuable tool for studying the implications of cathepsin L in pathophysiological conditions.
Cathepsin Inhibitor 3 is a selective inhibitor of the serine/threonine protease cathepsin S, functioning as a valuable tool in studying protease-mediated biological processes. This compound serves as a non-radioactive precursor in the synthesis of fluorine-18 radiolabeled compounds, facilitating research in molecular imaging. Additionally, Cathepsin Inhibitor 3 features an alkyne group, enabling its use in copper-catalyzed azide-alkyne cycloaddition (CuAAc), making it a versatile reagent for click chemistry applications in chemical biology.
Out of stock
All 3 sizes
Cathepsin-IN-5 is a selective inhibitor of cathepsins L and S, exhibiting IC50 values of 6.2 μM and 81 nM, respectively. This compound effectively inhibits cancer cell proliferation and induces apoptosis, while also reducing the growth of hepatocellular tumors in mouse models. Additionally, Cathepsin-IN-5 modulates the expression of genes associated with cell death and proliferation, making it a valuable reagent for research into hepatocellular carcinoma.
Out of stock
All 3 sizes