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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 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. -
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 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. -
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 C Inhibitor
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. -
Cathepsin A Substrate
FA-Phe-Phe is a furylacryloyl (fa)-amino acid derivative that serves as a specific substrate for Cathepsin A. This compound is valuable in elucidating the enzymatic activity and functional mechanisms of Cathepsin A, contributing to research on its role in physiological and pathological processes. FA-Phe-Phe is particularly useful in studies involving enzymatic assays and screening for potential inhibitors or modulators of Cathepsin A. -
Cathepsin L Inhibitor
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. -
Antimicrobial Peptide
Cathepsin G(1-5) is an antimicrobial peptide derived from the clostripain-digested cathepsin G mixture. This peptide exhibits significant antimicrobial activity, making it valuable for research on host defense mechanisms and the development of novel therapeutic agents. Cathepsin G(1-5) is utilized in studies exploring its effects on bacterial pathogens and potential applications in infection control. -
Cysteine Cathepsins Probe
DCG04 is an activity-based probe targeting cysteine cathepsins, serving as a multivalent ligand for the mannose-6-phosphate receptor. This compound enables the selective labeling of various cysteine cathepsins in cell and tissue lysates, facilitating the study of their roles in physiological and pathological processes. DCG04 is useful for researchers investigating enzyme activity and potential therapeutic interventions involving cysteine cathepsins. -
Cathepsin D Substrate
Bz-RGFFP-4MβNA is a specific substrate for Cathepsin D, designed for use in either colorimetric or fluorometric assays. It enables the detection and quantification of Cathepsin D activity, making it a valuable tool for studying proteolytic processes and their implications in various biological conditions. This compound facilitates research in areas including cancer, neurodegenerative diseases, and other pathologies where Cathepsin D plays a critical role. -
Substrate Peptide Of Cathepsin S
Ac-KQKLR-AMC is a substrate peptide designed for the fluorescent monitoring of Cathepsin S activity. Labeled with AMC, this compound exhibits excitation and emission wavelengths of 354 nm and 442 nm, respectively. It is primarily utilized in biochemical assays to measure the enzymatic activity of Cathepsin S, providing valuable insights into its role in physiological and pathological processes. -
Substrate Peptide Of Cathepsin S
Ac-KQKLR-AMC TFA is a substrate peptide for Cathepsin S, conjugated with the fluorescent indicator AMC (Excitation/Emission = 354 nm/442 nm). This reagent facilitates the measurement of Cathepsin S activity, enabling researchers to study proteolytic processes and assess enzyme function in various biological contexts. Its application is crucial for investigations into the role of Cathepsin S in physiological and pathological conditions. -
Cysteine Protease
Cathepsin S, human, is a potent cysteine protease that plays a crucial role in the degradation of damaged or harmful proteins within the endolysosomal pathway. This enzyme is implicated in various pathological processes, including arthritis, cancer, and cardiovascular diseases. Its activity makes it a valuable target for research applications aimed at understanding these diseases and developing therapeutic interventions. -
Ser/Thr Protease
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. -
Lysosomal cysteine protease
Cathepsin H, human liver, is a lysosomal cysteine protease that functions as both an aminopeptidase and an endopeptidase. This enzyme is essential for the catabolism of proteins within the lysosomal system. It plays a significant role in regulating tumor cell behavior and is implicated in the pathological processes of various brain diseases, making it valuable for research in cancer biology and neurodegenerative disorders. -
Biochemical Reagent
Cathepsin D (CTSD) is a lysosomal aspartic protease that plays a critical role in regulating lysosomal protease activity. Disruption of Cathepsin D function is associated with lysosomal dysfunction and the accumulation of proteins implicated in neurodegenerative diseases. Additionally, Cathepsin D is involved in the metastatic progression of breast cancer. This reagent is valuable for research applications related to cancer biology, neurodegeneration, and lysosomal disorders. -
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. -
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
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 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 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.

