Catalog No.
Product Name
Application
Product Information
Citations
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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 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 S inhibitor
Petesicatib is a cathepsin S inhibitor, used in research of immune diseases. -
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 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.- 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 C substrate
Gly-Phe-beta-naphthylamide is a cathepsin C substrate. The compound is described to accumulate inside lysosomes leading to their destruction. -
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 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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human cathepsin L inhibitor
Oxocarbazate, also known as CID23631927, is an inhibitor of human cathepsin L. -
Cathepsin L inhibitor
Z-FY-CHO (Z-Phe-Tyr-CHO) is a potent and specific inhibitor of cathepsin L (CTSL), a lysosomal cysteine protease involved in protein degradation and various pathological processes. It is commonly used as a tool compound in studies of CTSL-related functions and diseases. -
Cathepsin B Inhibitor
(Rac)-Z-FA-FMK is a potent inhibitor of cathepsin B, exhibiting a Ki value of 1.5 μM. This compound also inhibits multiple caspases, specifically caspases 2, 3, 6, 7, and 9, with IC50 values ranging from 6.147 to 110.7 μM. Additionally, (Rac)-Z-FA-FMK demonstrates antiviral activity by inhibiting the main protease involved in SARS-CoV-2 replication with an IC50 of 11.39 μM. It further attenuates the increase in IL-1β levels induced by LPS and represses NF-κB transactivation in macrophages, making it useful for research in inflammation and viral pathogenesis. -
Cysteine Protease
Cathepsin B, Bovine spleen is a cysteine protease that plays a critical role in various forms of programmed cell death, including apoptosis, pyroptosis, ferroptosis, necroptosis, and autophagic cell death. This enzyme is instrumental in research applications focused on understanding cellular mechanisms of death and disease progression. Additionally, it serves as a valuable tool for investigating proteolytic processes in both physiological and pathological contexts. -
Cathepsin Inhibitor
TS-24 is a selective inhibitor of cathepsin S, demonstrating an IC50 value of 4.3 μM. This compound has been shown to exhibit radiosensitizing effects in wild-type BRCA1 and triple-negative breast cancer (TNBC) xenograft models, primarily by inducing apoptotic pathways. TS-24 is suitable for research applications focused on cancer therapeutic development and understanding cathepsin-mediated biological processes. -
Cathepsin B/CANP Inhibitor
NCO-700 is a potent dual inhibitor of cathepsin B and calcium-activated neutral protease (CANP), exhibiting IC50 values of 0.8 μM and 46 μM, respectively. This compound effectively reduces myocardial fibrin degradation by inhibiting protease activity and demonstrates significant anti-tumor effects on hormone-independent cancer cells, including prostate cancer, by inducing apoptosis. NCO-700 serves as a valuable tool for investigating mechanisms underlying myocardial ischemia and exploring novel treatments for refractory hormone-independent tumors. -
Cathepsin L/JAK Inhibitor
Dual Cathepsin L/JAK-IN-1 is a dual inhibitor targeting Cathepsin L (CTSL) and Janus kinases (JAK), exhibiting IC50 values of 0.68 μM for CTSL, 337.1 nM for JAK1, 5.251 nM for JAK2, 27.29 nM for JAK3, and 172.6 nM for TYK2. This compound effectively inhibits the activation of key signaling pathways, including MAPK, NF-κB, and JAK/STAT, thereby providing substantial anti-inflammatory effects. Dual Cathepsin L/JAK-IN-1 is useful for investigating mechanisms underlying acute lung injury (ALI) and other inflammatory conditions. -
Cathepsin D/HSP90 Inhibitor
Tasiamide B is a potent inhibitor of Cathepsin D and HSP90, derived from the marine cyanobacteria Symploca sp. This linear peptide serves as a valuable scaffold for the development of inhibitors targeting aspartic proteases. Tasiamide B has demonstrated significant efficacy in skin cancer studies by effectively interacting with HSP90, highlighting its potential in cancer research and therapeutic applications. -
Cathepsin L Inhibitor
Cathepsin L-IN-6 is a selective inhibitor of cathepsin L, exhibiting an IC50 value of 0.021 μM. It functions by directly binding to cathepsin L, effectively suppressing its enzymatic activity. Additionally, Cathepsin L-IN-6 inhibits pro-inflammatory cytokines IL-6 and IL-8, demonstrating significant anti-inflammatory properties. This compound is particularly relevant for research focused on acute lung injury and related inflammatory conditions. -
Cathepsin Inhibitor
LV-320 is a potent uncompetitive inhibitor of cathepsin ATG4B, exhibiting an IC50 of 24.5 μM and a Kd of 16 μM. This compound effectively inhibits the enzymatic activity of ATG4B, thereby obstructing autophagic flux in cellular environments. Due to its stability and low toxicity, LV-320 is suitable for in vivo applications, making it a valuable tool for research on autophagy-related pathways. -
Cathepsin B Substrate
Z-Arg-Arg-AMC hydrochloride is a selective substrate for the cysteine protease cathepsin B. This compound is utilized in biochemical assays to monitor cathepsin B activity, making it essential for studying cellular processes such as protein degradation and apoptosis. Its application extends to cancer research and investigations into various diseases where cathepsin B is implicated. -
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 S Antagonist
RO5461111 is a highly specific and orally active antagonist of Cathepsin S, exhibiting IC50 values of 0.4 nM for human Cathepsin S and 0.5 nM for murine Cathepsin S. This compound effectively inhibits the activation of antigen-specific T cells and B cells, making it a valuable tool in immunological research. RO5461111 has shown potential in addressing pulmonary inflammation and lupus nephritis, highlighting its applicability in studying autoimmune diseases and related therapeutic interventions. -
Cathepsin L Substrate
Z-Phe-Arg-pNA is a selective substrate for Cathepsin L, facilitating the study of this cysteine protease's enzymatic activity. Upon cleavage by Cathepsin L, Z-Phe-Arg-pNA releases the chromogenic p-nitroaniline, allowing for quantification and real-time monitoring of protease activity. This compound is valuable for investigating the biochemical roles of Cathepsin L in various physiological processes and disease states. -
Cathepsin H Substrate
L-Arginine-7-amido-4-methylcoumarin hydrochloride is a specific substrate for cathepsin H, enabling studies into the enzyme's proteolytic activity. This compound does not serve as a substrate for cathepsins L and B, highlighting its selectivity. Its utility in biochemical assays facilitates research in fields such as cancer biology and lysosomal function, providing insights into cathepsin H's role in various physiological and pathological processes. -
Procathepsin Fluorogenic Substrate
Bz-FVR-AMC is a fluorogenic substrate specifically designed for the assay of procathepsin activity. With a kcat/Km value of 1070 mM^-1s^-1, it provides a robust tool for measuring cathepsin enzyme activity in various biological samples. Bz-FVR-AMC is particularly useful for studying proteolytic processes and understanding cysteine protease functions in both physiological and pathological contexts. However, at high concentrations, this substrate may exhibit inhibitory effects. -
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 C
Cathepsin C is a lysosomal cysteine protease that plays a crucial role in the catalytic activation of various serine proteases, including proteinase 3 (PR3), neutrophil elastase (NE), cathepsin G (CTSG), as well as granzymes A, B, and C, and mast cell chymase. This enzyme is vital for immune response regulation and has implications in inflammatory processes and cancer research. Cathepsin C serves as a valuable tool for studies involving protease activity and the mechanisms of disease related to immune cell function. -
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 B Substrate
Z-Arg-Arg-pNA is a substrate specifically designed for the detection of cathepsin B activity. It can be utilized in biochemical assays to measure the enzymatic function of cathepsin B, thereby aiding in research related to protease activity and related pathological conditions. This compound is valuable for studies focusing on cellular processes influenced by cathepsin B, including apoptosis and tissue remodeling. -
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. -
Human Platelet Activator
Cathepsin G is a potent agonist that targets human platelets, stimulating their activation and promoting aggregation. This enzyme plays a crucial role in hemostasis and inflammatory responses. It is valuable for research applications involving platelet biology and can be utilized in the screening of potential inhibitors that modulate platelet function. -
Cathepsin Substrate
N-CBZ-Phe-Arg-AMC is a specific substrate for lysosomal cathepsin enzymes, primarily utilized for assessing cathepsin activity. This compound exhibits fluorescent properties upon substrate cleavage, making it suitable for monitoring lysosomal protease activity in various biological samples. Its applications extend to studies on proteolytic processing and the role of cathepsins in cellular functions and disease states.
