Catalog No.
Product Name
Application
Product Information
Citations
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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. -
FXR Agonist
Cilofexor tromethamine is a nonsteroidal agonist of the farnesoid X receptor (FXR), primarily targeting liver diseases. It demonstrates significant potential in improving markers of cholestasis and liver injury, making it a valuable reagent in research for conditions such as primary sclerosing cholangitis. Cilofexor tromethamine has exhibited a favorable safety profile in clinical studies involving patients without cirrhosis, leading to notable enhancements in liver biochemical parameters and cholestatic markers. -
RAR/RXR
Ch55-O-C3-NH2 is a selective ligand for retinoic acid receptors (RAR) and retinoid X receptors (RXR). This compound demonstrates the ability to effectively modulate RAR signaling pathways, facilitating research into their role in gene expression and developmental processes. Ch55-O-C3-NH2 can also be utilized in the synthesis of SNIPERs by binding to cIAP1 ligand Bestatin through a linker, supporting studies in targeted protein degradation and therapeutic applications. -
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. -
NAMPT Degrader
NAMPT degrader-1 is an autophagosome-tethering compound (ATTEC) that targets nicotinamide phosphoribosyltransferase (NAMPT) with an IC50 of 0.023 μM. This compound effectively induces the degradation of NAMPT via the autophagy-lysosomal pathway, demonstrating significant antitumor activity in cellular models. NAMPT degrader-1 is valuable for research focused on cancer biology and the regulation of metabolic pathways involving NAD+ synthesis. -
PPAR Activator
Rosiglitazone sodium is a potent and selective activator of the peroxisome proliferator-activated receptor gamma (PPARγ), exhibiting EC50 values of 30 nM, 100 nM, and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively, with a Kd of approximately 40 nM. In addition to its role as a PPARγ activator, Rosiglitazone sodium functions as a modulator of transient receptor potential (TRP) channels, specifically inhibiting TRP melastatin 2 (TRPM2) and TRPM3, while activating TRP canonical 5 (TRPC5). This compound is utilized in research related to metabolic disorders, obesity, and other conditions linked to PPARγ signaling. -
RAR/RXR Agonist
Acitretin sodium functions as a retinoic acid receptor (RAR) and retinoid X receptor (RXR) agonist. Primarily utilized in the treatment of psoriasis, this second-generation systemic retinoid also shows potential in the research of Alzheimer's disease. Its ability to modulate gene expression and influence cellular differentiation makes it a valuable tool for investigating retinoid signaling pathways in various biological contexts. -
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 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. -
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.
