Cathepsin

Cat. No.

A39780

CAS No.

108005-94-3

Cathepsin L-IN-2

Synonyms: (Rac)-Z-Phe-Phe-FMK

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.

Cat. No.

A39781

CAS No.

110115-07-6

ALLM

Synonyms: Calpain inhibitor II

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.

Cat. No.

A39782

CAS No.

2418577-51-0

Cathepsin X-IN-1

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.

Cat. No.

A39784

CAS No.

262381-84-0

JPM-OEt

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.

Cat. No.

A39785

CAS No.

56121-42-7

Aurantiamide acetate

Synonyms: Asperglaucide

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.

Cat. No.

A39786

CAS No.

1131456-28-4

KGP94

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.

Cat. No.

A39787

CAS No.

105608-85-3

Z-FF-FMK

Synonyms: Z-Phe-Phe-FMK

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.

Cat. No.

A39789

CAS No.

362505-84-8

Relacatib

Synonyms: SB-462795

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.

Cat. No.

A39790

CAS No.

2825567-97-1

Cathepsin C-IN-5

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.

Cat. No.

A39796

CAS No.

1628521-28-7

CatD-IN-1

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.

Cat. No.

A39797

CAS No.

2565572-83-8

AEP-IN-2

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.

Cat. No.

A39799

CAS No.

1613458-78-8

GSK-2793660

GSK-2793660 is an orally active and irreversible inhibitor of Cathepsin C (CTSC). This compound demonstrates significant potential for investigating the role of CTSC in bronchiectasis and related conditions. Its efficacy as a CTSC inhibitor makes it a valuable tool for exploring therapeutic approaches aimed at modulating inflammation and tissue remodeling in respiratory diseases.

Cat. No.

A39800

CAS No.

1017931-53-1

Cathepsin Inhibitor 2

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.

Cat. No.

A39802

CAS No.

868273-90-9

ONO-5334

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.

Cat. No.

A39803

CAS No.

14080-23-0

2-Cyanopyrimidine

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.

Cat. No.

A39805

CAS No.

989-30-0

3-Epiursolic Acid

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.

Cat. No.

A39811

CAS No.

114014-15-2

Z-Phe-Tyr(tBu)-diazomethylketone

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.

Cat. No.

A39814

CAS No.

1627094-88-5

Gü2602

Gü2602 is a highly selective, reversible inhibitor of cathepsin K (CatK) with a Ki value of 0.013 nM for mature CatK (mCatK). This compound effectively inhibits the autocatalytic activation of the cathepsin K zymogen, making it a valuable tool for studying osteoclastogenesis and bone resorption. Gü2602 is applicable in research areas focused on osteoporosis, cancer metastasis, and other diseases related to abnormal bone remodeling.

Cat. No.

A39816

CAS No.

1613458-70-0

GSK-2793660 free base

GSK-2793660 free base is an oral, irreversible inhibitor of Cathepsin C (CTSC). This compound exhibits potent inhibitory activity, making it a valuable tool for researching conditions linked to CTSC, such as bronchiectasis. Its unique mechanism of action enables the exploration of therapeutic strategies targeting CTSC in various pathological settings.

Cat. No.

A39821

CAS No.

250584-13-5

Z-DEVD-CMK

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.

Cat. No.

A39822

CAS No.

518062-14-1

JNJ-10311795

Synonyms: RWJ-355871

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.

Cat. No.

A39823

CAS No.

161709-56-4

Cathepsin L-IN-4

Synonyms: 1-Naphthalenesulfonyl-Ile-Trp-CHO

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.

Cat. No.

A39827

CAS No.

433212-75-0

SSAA09E1

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.

Cat. No.

A39828

CAS No.

65178-14-5

Z-Phe-Phe-Diazomethylketone

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. No.

A39830

CAS No.

325775-42-6

Cathepsin K inhibitor 6

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.