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Cathepsin S inhibitor
Z-FL-COCHO (LY3000328) is a novel Cathepsin S inhibitor.
- Gil-Im Mun, .et al. , Biochim Biophys Acta Mol Basis Dis, 2024, Sep 25;1871(1):167523 PMID: 39332782
- Fu R, .et al. , Sci Rep, 2020, Jan 29;10(1):1455 PMID: 31996771
- Klinngam W, .et al. , Sci Rep, 2019, Jul 2;9(1):9559 PMID: 31267034
- Chen CY, .et al. , Clin Sci (Lond), 2018, Oct 29;132(20):2221-2239 PMID: 30287519
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cathepsin inhibitor
VBY-825 is a novel, reversible cathepsin inhibitor with high potency against cathepsins B, L, S and V.- Laura Odongo, .et al. , Microbiol Spectr, 2023, Sep 20;11(5):e0190823 PMID: 37728342
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Cathepsin B inhibitor
CA-074 methyl ester is a cell-permeable analog of CA-074 that acts as an irreversible cathepsin B inhibitor. CA-074 methyl ester is reported to inhibit bone resorption in rodent models and shown to inhibit B16 melanoma cell invasion in vitro.- Maohuan Ran, .et al. , Ecotoxicol Environ Saf, 2026, May:316:120163 PMID: 42013791
- Qian Chu, .et al. , Food Chem Toxicol, 2021, Jan;147:111867 PMID: 33217525
- Ye Tao, .et al. , Chemosphere, 2020, Mar;242:124959 PMID: 31669990
- Ming Sun, .et al. , J Agric Food Chem, 2018, Nov 21;66(46):12376-12384 PMID: 30392375
- Xueyan Wu, .et al. , Food Chem Toxicol, 2017, Aug;106(Pt A):273-282 PMID: 28579546
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Cathepsin B inhibitor
CA-074 is a potent inhibitor of cathepsin B with a Ki of 2 to 5 nM.- Tianming Qiu, .et al. , Cell Death Dis, 2018, Oct; 9(10): 946 PMID: 30237538
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Cathepsin K Inhibitor
Odanacatib is an inhibitor of cathepsin K,an enzyme involved in bone resorption. -
Cathepsin Inhibitor
Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively. -
cathepsin S inhibitor
Petesicatib is a cathepsin S inhibitor, used in research of immune diseases. -
human cathepsin L inhibitor
Oxocarbazate, also known as CID23631927, is an inhibitor of human cathepsin L. -
Human cathepsin L inhibitor
SID 26681509 is a reversible and potent human cathepsin L inhibitor. SID 26681509 displays no inhibitory activity of cathepsin G. -
Cathepsin G Inhibitor
Cathepsin G Inhibitor I is a potent and selective reversible competitive inhibitor of Cathepsin G, exhibiting an IC50 value of 53 nM and a Ki of 63 nM. This non-peptidic compound is primarily utilized in research investigating immune disorders, providing valuable insights into the role of Cathepsin G in various pathogenic processes. Its specificity makes it a useful tool for understanding the implications of Cathepsin G in immune system regulation. -
Cathepsin L Inhibitor
Cathepsin L-IN-2 is a selective inhibitor of Cathepsin L, exhibiting an IC50 of 15 μM. This compound irreversibly inhibits the proteolytic activity of cathepsins by covalently binding to cysteine residues in the enzyme's active site. Cathepsin L-IN-2 is primarily utilized in research focused on neurodegenerative diseases, including GRN-related frontotemporal dementia, as well as in studies investigating cancer invasion and metastasis. -
Calpain/Cathepsin Inhibitor
ALLM, also known as Calpain inhibitor II, acts as a potent inhibitor of calpain and cathepsin proteases. This compound is known to mitigate neuronal cell death, thereby enhancing chronic neurological function following spinal cord injury (SCI). Its utility in research extends to studies investigating protease activity and the mechanisms underlying neuroprotection in trauma-related conditions. -
Cathepsin X Inhibitor
Cathepsin X-IN-1 is a potent inhibitor of Cathepsin X, exhibiting an IC50 of 7.13 µM. This compound effectively reduces PC-3 cell migration while demonstrating low cytotoxicity. It serves as a valuable tool in cancer research, particularly in studies focused on metastatic processes and the modulation of proteolytic enzymes. -
Cysteine Cathepsin Inhibitor
JPM-OEt is a potent cysteine cathepsin inhibitor that binds covalently to the active site, irreversibly inhibiting the cysteine cathepsin family. This compound demonstrates significant antitumor activity, making it a valuable tool for cancer research. Its ability to modulate cysteine cathepsins expands its potential applications in studying various pathophysiological processes and therapeutic interventions. -
Cathepsin Inhibitor
Aurantiamide acetate is a selective and orally active inhibitor of cathepsins, derived from the plant Portulaca oleracea L. This compound exhibits significant anti-inflammatory properties, making it valuable for investigating the mechanisms underlying inflammatory diseases. Researchers can utilize aurantiamide acetate to explore therapeutic strategies aimed at modulating cathepsin activity in various pathological conditions. -
Cathepsin L Inhibitor
KGP94 is a selective inhibitor of cathepsin L, exhibiting an IC50 value of 189 nM. This compound effectively inhibits the migration and invasion of metastatic carcinoma while demonstrating low cytotoxicity with a GI50 of 26.9 µM across various human cell lines. KGP94 is suitable for research applications focused on cancer biology and the modulation of proteolytic enzyme activity. -
Cathepsin-L Inhibitor
Z-FF-FMK is a selective inhibitor of cathepsin L, primarily known for its role in regulating apoptotic processes. This compound effectively prevents β-amyloid-induced apoptotic changes, including the activation of caspase-3, cleavage of poly-ADP ribose polymerase, and subsequent DNA fragmentation. Z-FF-FMK is valuable in research applications focused on neurodegenerative diseases and the role of proteolytic enzymes in apoptosis. -
Cathepsins Inhibitor
Relacatib is a potent, orally active inhibitor of human cathepsins K, L, and V, demonstrating Ki values of 41 pM, 68 pM, and 53 pM, respectively. This compound effectively inhibits endogenous cathepsin K in situ within human osteoclasts, significantly impacting osteoclast-mediated bone resorption with IC50 values of 45 nM and 70 nM. Relacatib shows promise in preclinical research for reducing bone resorption both in vitro using human tissue and in vivo studies in cynomolgus monkeys. -
Cathepsin C Inhibitor
Cathepsin C-IN-5 is a selective inhibitor of Cathepsin C, exhibiting an IC50 of 59.9 nM, with minimal activity against other cathepsins such as Cat L (4.26 µM) and others (>5 µM). This compound effectively inhibits Cathepsin C activity in bone marrow and blood, leading to a reduction in the activation of neutrophil serine proteases (NSPs). Its anti-inflammatory properties make Cathepsin C-IN-5 a valuable tool for research exploring inflammatory disorders and related pathways. -
Cathepsin D Inhibitor
CatD-IN-1 is a selective inhibitor of cathepsin D, demonstrating an IC50 of 0.44 μM. This compound serves as a valuable tool for investigating the biochemical pathways involved in osteoarthritis research. Its specific inhibition of cathepsin D may facilitate studies on tissue remodeling and degeneration associated with joint diseases. -
AEP Inhibitor
AEP-IN-2 is an inhibitor of asparagine endopeptidase (AEP), effectively blocking the cleavage of amyloid precursor protein (APP) and tau protein. This compound exhibits oral bioactivity and is capable of reducing levels of amyloid beta 40 (Aβ40), amyloid beta 42 (Aβ42), and phosphorylated tau (p-Tau). AEP-IN-2 is utilized in research applications focused on neurodegenerative diseases and the modulation of protein aggregation pathways. -
Cathepsin Inhibitor
Cathepsin Inhibitor 2 is a highly potent inhibitor of Cathepsin S, exhibiting a Ki value of less than 20 nM. This compound is primarily utilized in research to investigate the role of cathepsins in various biological processes, including protein degradation and immune responses. It serves as a valuable tool for studies related to cancer, inflammation, and other conditions where Cathepsin S activity is a contributing factor. -
Cathepsin K Inhibitor
ONO-5334 is a potent and selective inhibitor of cathepsin K, exhibiting Ki values of 0.10 nM, 0.049 nM, and 0.85 nM for human, rabbit, and rat cathepsin K, respectively. This compound also demonstrates significant antiviral activity against SARS-CoV-2, with an EC50 value of 500 nM. ONO-5334 is valuable for research applications involving osteoporosis and COVID-19, facilitating the exploration of therapeutic interventions targeting these conditions. -
Cysteine Protease Cathepsin K Inhibitor
2-Cyanopyrimidine is a potent inhibitor of cysteine protease cathepsin K, exhibiting an IC50 value of 170 nM. This compound demonstrates significant biological activity in the modulation of bone resorption and is being investigated for its potential therapeutic applications in osteoporosis. Researchers can utilize 2-Cyanopyrimidine to study the role of cathepsin K in bone metabolism and related disorders. -
Cathepsin L Inhibitor
3-Epiursolic Acid is a triterpenoid compound that functions as a competitive inhibitor of cathepsin L, demonstrating an IC50 value of 6.5 μM and a Ki value of 19.5 μM. This compound exhibits selectivity for cathepsin L without significantly affecting cathepsin B. Its inhibitory properties make it valuable for research into protease inhibition and related biological pathways. -
Cathepsin L Inhibitor
Z-Phe-Tyr(tBu)-diazomethylketone is a potent inhibitor of cathepsin L, an enzyme involved in various cellular processes. This compound has been shown to facilitate the disassembly of reovirus, thereby reducing viral detection levels. It serves as a valuable tool in research applications targeting viral infections and evaluating the role of cathepsin L in disease mechanisms. -
Cathepsins Inhibitor
Z-DEVD-CMK is an irreversible inhibitor targeting cathepsins, demonstrating potent activity against various cathepsin isoforms in vitro. This compound is utilized in research to study the role of cathepsins in apoptosis, inflammation, and cancer progression. It serves as a valuable tool for elucidating the functional mechanisms of cathepsins in biological systems. -
Cathepsin G/Chymase Inhibitor
JNJ-10311795 is a potent dual inhibitor targeting neutrophil cathepsin G (Ki = 38 nM) and mast cell chymase (Ki = 2.3 nM). This compound demonstrates significant anti-inflammatory properties, making it valuable for research aimed at elucidating the roles of these proteases in inflammatory diseases. Its specificity and efficacy render it suitable for studies focused on developing therapeutics for conditions associated with excessive inflammation. -
Cathepsin L Inhibitor
Cathepsin L-IN-4 is a potent inhibitor of cathepsin L, demonstrating an IC50 in the nanomolar range. This compound effectively attenuates the activity of cathepsin L, which is involved in various pathological processes, including cancer progression and inflammatory responses. Cathepsin L-IN-4 can be utilized in research applications aimed at elucidating the role of cathepsin L in disease models and therapeutic interventions. -
Cathepsin L Inhibitor
SSAA09E1 is a selective inhibitor of cathepsin L, with an IC50 of 5.33 μM. This compound effectively blocks critical stages of viral entry and has been employed in research focused on SARS-CoV infection. Its role in modulating cathepsin L activity makes it a valuable tool for investigating therapeutic strategies against viral pathogens. -
Cathepsin Inhibitor
Z-Phe-Phe-Diazomethylketone is a selective inhibitor of cathepsin L, a cysteine protease involved in various cellular processes. This compound exhibits significant inhibitory activity toward cathepsin L, making it valuable in studies related to protein degradation, apoptosis, and various pathological conditions such as cancer and inflammation. It is useful for research applications that require modulation of proteolytic pathways involving cathepsins. -
Cat K Inhibitor
Cathepsin K inhibitor 6 is a potent small molecule specifically targeting cathepsin K (Cat K) with an IC50 value of 17 nM. In addition to its primary activity, it also demonstrates inhibitory effects on cathepsin L and cathepsin B, with IC50 values of 0.05 μM and 0.3 μM, respectively. This compound is valuable for studying bone resorption, fibrosis, and various pathological conditions associated with cathepsin activity. -
Cathepsin K Inhibitor
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. -
Cathepsin L Inhibitor
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. -
Cathepsin B Inhibitor
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. -
Cathepsin C Inhibitor
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. -
Cathepsin S Inhibitor
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
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. -
Cathepsin L Inhibitor
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. -
Cathepsin L Inhibitor
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. -
Cathepsin Inhibitor
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. -
Cathepsin E Inhibitor
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. -
Cysteine Cathepsin Inhibitor
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. -
Cathepsin S Inhibitor
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.

