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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. -
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. -
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. -
Cathepsin B Specific Substrate
Z-Arg-Arg-βNA acetate is a selective dipeptide substrate for the protease Cathepsin B, exhibiting resistance to proteases H and L. This compound plays a crucial role in differentiating Cathepsin B from other proteases, making it a valuable tool for research focused on protease activity and function. Its sensitivity allows for precise monitoring of Cathepsin B activity in various biological assays. -
Cathepsin K
Cathepsin K is a cysteine protease that exhibits endopeptidase and collagenolytic activities. It plays a crucial role in the degradation of collagen in bone tissue, making it a significant target in osteoporosis research. Studies of Cathepsin K contribute to understanding bone remodeling processes and the development of therapeutic strategies for bone-related diseases. -
Cathepsin B Substrate
Arg-Arg-AMC is a selective substrate for Cathepsin B, an enzyme implicated in various cancer progression pathways. This reagent is valuable for assessing Cathepsin B activity in cancer cell models, where its expression is associated with invasive and metastatic characteristics. Its application in research can facilitate the investigation of tumor biology and potential therapeutic targets related to Cathepsin B. -
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 S Substrate
Z-Leu-Leu-Arg-AMC is a synthetic peptide substrate specifically designed for cathepsin S. This compound serves as a fluorogenic substrate, enabling the measurement of cathepsin S activity in various biological samples. It is utilized in research applications focusing on protease activity, cellular degradation processes, and the study of lysosomal function and related diseases. -
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 D/E FRET Substrate
Cathepsin D and E FRET Substrate is a fluorogenic substrate specifically designed for the selective detection of cathepsins D and E, avoiding interaction with cathepsins B, H, and L. Cleavage occurs at the Phe-Phe amide bond, releasing a fluorescent signal that can be quantitatively measured. This substrate is ideal for routine assays and mechanistic studies, facilitating the investigation of cathepsin activity in various biological contexts. -
Cathepsin D Substrate
Ac-Glu-Asp(EDANS)-Lys-Pro-Ile-Leu-Phe-Phe-Arg-Leu-Gly-Lys(DABCYL)-Glu-NH2 is a specific substrate for cathepsin D, designed for use in fluorescence resonance energy transfer (FRET) assays. This compound exhibits key biological activity by releasing a detectable fluorescence signal upon cathepsin D cleavage, facilitating the study of proteolytic activity. It is valuable for investigating the role of cathepsin D in various biological processes and for screening potential inhibitors in drug development. -
Cathepsin
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. -
Cathepsin G Substrate
Suc-Val-Pro-Phe-pNA functions as a substrate specifically for cathepsin G. This compound allows for the quantitative assessment of cathepsin G activity, which is crucial for understanding its role in various physiological and pathological processes. Its application includes enzyme activity assays in research focused on inflammation, immune response, and other related biological pathways. -
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 B Substrate
Z-Arg-Arg-4MβNA triacetate is a specific substrate for cathepsin B, designed to facilitate the study of this cysteine protease. Upon cleavage by cathepsin B, it generates the fluorescent product 4MβNA, which exhibits excitation and emission maxima at 355 nm and 430 nm, respectively. This reagent is useful for investigating enzyme activity and dynamics in various biological research applications. -
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. -
Cathepsin C Inhibitor
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. -
Cathepsin C Inhibitor
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. -
Cathepsin K Inhibitor
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. -
Cathepsin
Heterophyllin A is a natural compound that targets cathepsin enzymes. This compound exhibits notable biological activity by inhibiting cathepsin protease activity, making it a valuable reagent for research into proteolytic pathways. Its applications include studies on cellular processes related to protein degradation, as well as potential therapeutic investigations regarding disease states linked to dysregulated cathepsin function.

