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FAAH Inhibitor
N-Benzyllinolenamide is a natural macamide derived from Lepidium meyenii and acts as an inhibitor of fatty acid amide hydrolase (FAAH) with an IC50 value of 41.8 μM. This compound is valuable for studying the modulation of endocannabinoid signaling pathways and investigating the role of FAAH in various physiological processes. Its ability to inhibit FAAH makes it a useful tool in research related to pain management, inflammation, and neuroprotection. -
HMG-CoA Reductase Inhibitor
(3R,5S)-Fluvastatin sodium is a potent competitive inhibitor of HMG-CoA reductase, displaying an IC50 value of 8 nM. This compound is effective in modulating lipid levels and exhibits protective effects on vascular smooth muscle cells by activating the Nrf2-dependent antioxidant pathway, mitigating oxidative stress. It is widely utilized in cardiovascular research and studies focusing on cholesterol metabolism and oxidative stress responses. -
HMG-CoA Reductase Inhibitor
(3R,5R)-Rosuvastatin is a competitive inhibitor of HMG-CoA reductase, exhibiting an IC50 value of 11 nM. This compound is known for its ability to significantly reduce levels of low-density lipoprotein (LDL) cholesterol, triglycerides, and C-reactive protein. Additionally, (3R,5R)-Rosuvastatin has been shown to inhibit human ether-a-go-go related gene (hERG) currents with an IC50 of 195 nM, impacting hERG protein expression and its interactions with heat shock protein 70 (Hsp70). Its pharmacological profile makes it valuable for research related to cholesterol management and cardiovascular health. -
HMG-CoA Reductase Inhibitor
(3S,5R)-Rosuvastatin is a competitive inhibitor of HMG-CoA reductase, exhibiting an IC50 of 11 nM. This agent plays a significant role in reducing low-density lipoprotein (LDL) cholesterol and triglyceride levels while decreasing C-reactive protein levels. Additionally, (3S,5R)-Rosuvastatin inhibits the hERG channel with an IC50 of 195 nM and modulates the expression of the hERG protein through the disruption of its interaction with heat shock protein 70 (Hsp70). This compound is valuable in cardiovascular research and studies focused on cholesterol metabolism. -
HMG-CoA Reductase Inhibitor
(3S,5R)-Fluvastatin-d6 is a deuterium-labeled derivative of the HMG-CoA reductase inhibitor, Fluvastatin. As a competitive inhibitor with an IC50 of 8 nM, it effectively regulates cholesterol biosynthesis. This compound has been shown to protect vascular smooth muscle cells from oxidative stress via the Nrf2-dependent antioxidant pathway, making it a valuable tool in cardiovascular research and studies focused on oxidative damage and cellular stress responses. -
CYP2C9/CYP3A4 Inhibitor
Tetrahydrocurcumin-d6 is a deuterated analog of Tetrahydrocurcumin, functioning as an inhibitor of CYP2C9 and CYP3A4 enzymes. This compound exhibits significant biological activity against these cytochrome P450 isoforms, making it valuable for research into drug metabolism and pharmacokinetics. Tetrahydrocurcumin-d6 is utilized in studies aiming to elucidate the metabolic pathways and interactions of curcuminoids, as well as their potential therapeutic applications. -
HMG-CoA Reductase Inhibitor
Atorvastatin strontium is an HMG-CoA reductase inhibitor that effectively lowers cholesterol levels, impacting cardiovascular health. Its primary mechanism involves the inhibition of HMG-CoA reductase in liver tissue, which plays a crucial role in cholesterol synthesis. This compound is also utilized in research to address dyslipidemia and related metabolic disorders. -
FAAH Inhibitor
SA72 is a highly selective inhibitor of fatty acid amide hydrolase (FAAH), an enzyme crucial for the degradation of endocannabinoids. By inhibiting FAAH, SA72 modulates endocannabinoid levels, leading to potential therapeutic effects in pain management and inflammation. This compound serves as a valuable tool in research aimed at understanding the endocannabinoid system and its role in various physiological processes. -
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. -
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 K inhibitor
Cathepsin K inhibitor 5 is a selective inhibitor of Cathepsin K, a cysteine protease involved in bone resorption and remodeling. This compound effectively inhibits Cathepsin K activity, making it valuable for studying osteoclast function and bone-related diseases such as osteoporosis. Its use in research can enhance understanding of bone metabolism and aid in the development of novel therapeutic strategies for bone disorders. -
Cathepsin D inhibitor
TB-9 is a potent inhibitor of cathepsin D, cathepsin E, and BACE1, exhibiting IC50 values of 0.0783 nM, 0.724 nM, and 54.2 nM, respectively. This compound shows significant potential in the study of neurodegenerative diseases and cancer, where cathepsin activity is implicated. Its ability to selectively target these enzymes makes TB-9 an important tool for researchers investigating the role of proteases in various biological processes. -
Cathepsin K Inhibitor
Cathepsin K-IN-8 is a potent inhibitor of cathepsin K, an enzyme involved in the degradation of extracellular matrix components. This compound is primarily utilized in research focused on inflammatory diseases such as rheumatoid arthritis and osteoarthritis, as well as conditions like osteoporosis and tumor progression. Its inhibition of cathepsin K allows for the investigation of its role in these pathological processes, making it a valuable tool for studying bone resorption and related disorders. -
Cathepsin S Inhibitor
BI-1124 is a selective inhibitor of cathepsin S, a cysteine protease involved in various pathological processes, including inflammation and tissue remodeling. This compound demonstrates effective ocular pharmacokinetic-pharmacodynamic properties in rabbit models following topical administration. BI-1124 is primarily utilized in research focused on age-related dry eye disease, making it a valuable tool for exploring therapeutic interventions in ocular health.

