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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.
Leupeptin is a membrane-permeable broad-spectrum protease inhibitor that effectively targets serine, cysteine, and threonine proteases. This compound has been shown to inhibit the main protease of SARS-CoV-2 (Mpro) while also exhibiting anti-inflammatory properties. Leupeptin is valuable for research applications involving proteolytic processes and can aid in the study of viral infections and inflammatory responses.
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Z-Leu-Tyr-Chloromethylketone is a potent inhibitor of cathepsins, a family of cysteine proteases involved in various cellular processes. This compound exhibits significant inhibitory activity, making it valuable for studies related to protein degradation and apoptotic signaling pathways. It is applicable in research exploring the roles of cathepsins in diseases such as cancer and neurodegeneration.
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MK 1256 is a highly selective and orally active inhibitor of cathepsin K (Cat K) with an IC50 value of 0.62 nM. It demonstrates exceptional selectivity towards other tissue proteases, being over 1100 times more selective, and shows a moderate selectivity for cathepsin F (Cat F) at 110 times. MK 1256 effectively inhibits bone resorption in ovariectomized rhesus monkeys, making it a valuable tool for osteoporosis research.
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Cathepsin K inhibitor 2 is a selective inhibitor targeting cathepsin K, a cysteine protease implicated in collagen degradation and bone remodeling. Inhibition of cathepsin K is particularly relevant in the study of osteoporosis and osteoarthritis, as it plays a crucial role in these conditions. This compound provides a valuable tool for researchers investigating the molecular mechanisms underlying bone-resorptive diseases and developing potential therapeutic strategies.
RKLLW-NH2 is a selective inhibitor of Cathepsin L, a cysteine protease involved in various physiological and pathological processes. This compound exhibits significant inhibitory activity, making it a valuable tool for research focused on cancer, inflammation, and autoimmune diseases. RKLLW-NH2 may aid in elucidating the role of Cathepsin L in different biological pathways and conditions.
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Ac-Leu-Val-Lys-Aldehyde is a highly effective inhibitor of cathepsin B, demonstrating an IC50 of 4 nM. This compound exhibits significant neuroprotective activity by reducing quinolinic acid-induced striatal cell death and promoting the accumulation of LC3-II, a marker associated with autophagy. It serves as a valuable tool for investigating the role of cathepsin B in various biological processes and potential therapeutic strategies for neurodegenerative diseases.
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Cathepsin C-IN-4 is a selective inhibitor targeting Cathepsin C, demonstrating a potent inhibitory activity with an IC50 of 65.6 nM. In addition to its primary action, Cathepsin C-IN-4 exhibits significant inhibition in THP-1 and U937 cell lines with IC50 values of 203.4 nM and 177.6 nM, respectively. This compound is valuable for studies exploring the role of Cathepsin C in various biological processes and associated diseases.
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Gü1303 is a potent, reversible inhibitor of cathepsin K (CatK) that demonstrates a Ki of 0.91 nM for mature CatK (mCatK). This compound effectively suppresses the autocatalytic activation of the cathepsin K zymogen, making it valuable for studies related to bone resorption and various pathological conditions associated with CatK activity. Gü1303 is suitable for research applications in the fields of enzymology, pharmacology, and disease modeling.
JNJ 10329670 is a selective noncovalent inhibitor of cathepsin S, exhibiting a Ki value of 34 nM for human cathepsin S. This compound effectively inhibits invariant chain proteolysis in B cells and dendritic cells, leading to the modulation of antigen-induced T cell proliferation. It serves as a valuable tool in immunological research and studies focused on autoimmune diseases and cancer immunotherapy.
Cathepsin K Inhibitor 3 is a highly selective inhibitor targeting cathepsin K, demonstrating an IC50 value of 0.5 nM. This compound exhibits a favorable pharmacokinetic profile, making it suitable for research applications in osteoarthritis studies. Its specific action on cathepsin K positions it as a valuable tool in elucidating the role of this enzyme in bone resorption and related conditions.
CLIK-148 is a highly selective, irreversible inhibitor of Cathepsin L, a cysteine protease known for its role in protein degradation. This compound effectively prevents the Cathepsin L-mediated degradation of HMG-CoA reductase within the endoplasmic reticulum and inhibits the processing of proCCK, subsequently reducing CCK8 production. CLIK-148 also impairs the breakdown of type I collagen by osteoclast-secreted Cathepsin L, thereby mitigating tumor-induced bone metastasis and hypercalcemia. This compound is valuable for investigating bone metabolism disorders and neuropeptide processing regulation.
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Cathepsin L-IN-3 is a selective noncovalent inhibitor of cathepsin L, exhibiting a Ki value of 4.3 nM. This compound effectively modulates cathepsin L activity, making it a valuable tool for studies in cancer biology and inflammation. Its potency and selectivity enable researchers to investigate the role of cathepsin L in various physiological and pathological processes.
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ABP 25 is an activity-based probe specifically designed to inhibit cathepsin K, demonstrating high potency and selectivity. This reagent enables effective imaging of cathepsin K activity, making it a valuable tool for studying diseases where cathepsin K plays a critical role, such as bone resorption and related pathologies. Its application extends to various research fields, including cancer, osteoporosis, and cardiovascular diseases.
SQ 32056 is a potent inhibitor of cathepsin E, an aspartyl protease involved in various biological processes, including immune response and inflammation. This compound effectively obstructs the pressor response to endothelin, making it a valuable tool for research into cardiovascular and inflammatory diseases. Its applications extend to studying the role of cathepsins in pathological conditions and evaluating therapeutic strategies targeting protease-mediated signaling pathways.
GB111-NH2 is a potent cysteine cathepsin inhibitor that plays a crucial role in the modulation of proteolytic activity associated with various pathological conditions, including cancer. Its inhibitory action on cathepsins has made it a valuable tool for researchers investigating tumor progression and metastasis. This compound can facilitate the understanding of cysteine cathepsin's role in cancer biology and aid in the development of targeted therapies.
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BI-1915 is a selective inhibitor of Cathepsin S, exhibiting an IC50 of 17 nM. This compound is valuable for studying the role of Cathepsin S in autoimmune diseases and may aid in the development of therapeutic strategies targeting these conditions. Its specificity makes it a useful tool for dissecting the biological functions of this enzyme in various research applications.
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Cathepsin C-IN-3 is a selective inhibitor of Cathepsin C, demonstrating a potency with an IC50 value of 61.79 nM. This compound effectively inhibits the proliferation of THP-1 and U937 cell lines, with IC50 values of 101.5 nM and 86.5 nM, respectively. Cathepsin C-IN-3 is valuable for studies focused on the role of Cathepsin C in inflammation and immune responses.
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Cathepsin C-IN-7 is a selective inhibitor of Cathepsin C, an enzyme implicated in various inflammatory and cancer-related processes. This compound demonstrates significant biological activity in modulating immune responses and has potential applications in the study of primary cancers and cancer metastases. Researchers can utilize Cathepsin C-IN-7 to investigate the role of Cathepsin C in tumor biology and the progression of malignancies.
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MV061194 is a selective inhibitor of cathepsin K, exhibiting a human Ki of 2.5 nM. This compound is utilized in research focused on osteoporosis, providing insights into bone resorption processes and potential therapeutic strategies for bone-related disorders. Its specificity and potency make it a valuable tool for studying the role of cathepsin K in various biological contexts.
CAA-0225 is a selective inhibitor of the tissue protease L, specifically targeting TbCATL with an IC50 of 1.9 nM. This compound has demonstrated significant biological activity, including the degradation of autophagosome membrane markers such as LC3-II and GABARAP. Additionally, CAA-0225 improves cardiac function in models of reperfusion injury and exhibits efficacy against Trypanosoma brucei, highlighting its potential applications in cardiovascular research and parasitology studies.
Cathepsin K inhibitor 5 is a selective inhibitor of Cathepsin K, a cysteine protease involved in bone resorption and remodeling. This compound effectively inhibits Cathepsin K activity, making it valuable for studying osteoclast function and bone-related diseases such as osteoporosis. Its use in research can enhance understanding of bone metabolism and aid in the development of novel therapeutic strategies for bone disorders.
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TB-9 is a potent inhibitor of cathepsin D, cathepsin E, and BACE1, exhibiting IC50 values of 0.0783 nM, 0.724 nM, and 54.2 nM, respectively. This compound shows significant potential in the study of neurodegenerative diseases and cancer, where cathepsin activity is implicated. Its ability to selectively target these enzymes makes TB-9 an important tool for researchers investigating the role of proteases in various biological processes.
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Cathepsin K-IN-8 is a potent inhibitor of cathepsin K, an enzyme involved in the degradation of extracellular matrix components. This compound is primarily utilized in research focused on inflammatory diseases such as rheumatoid arthritis and osteoarthritis, as well as conditions like osteoporosis and tumor progression. Its inhibition of cathepsin K allows for the investigation of its role in these pathological processes, making it a valuable tool for studying bone resorption and related disorders.
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BI-1124 is a selective inhibitor of cathepsin S, a cysteine protease involved in various pathological processes, including inflammation and tissue remodeling. This compound demonstrates effective ocular pharmacokinetic-pharmacodynamic properties in rabbit models following topical administration. BI-1124 is primarily utilized in research focused on age-related dry eye disease, making it a valuable tool for exploring therapeutic interventions in ocular health.
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Z-FG-NHO-Bz is a selective inhibitor of cathepsins, a family of cysteine proteases involved in various biological processes. This compound exhibits significant inhibitory activity against cathepsin B and L, making it a valuable tool for studying their roles in pathological conditions such as cancer and neurodegenerative diseases. Z-FG-NHO-Bz is ideal for research applications focused on proteolytic enzyme regulation and therapeutic intervention.
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