Catalog No.
Product Name
Application
Product Information
Citations
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Substrate For The Trypsin-like Activity Of 20S Proteasome
Bz-VGR-AMC is a synthetic substrate specifically designed for the trypsin-like activity of the 20S proteasome. This compound enables the quantification of β2 activity within the proteasome, serving as a valuable tool for researching proteasomal function and regulation. Its application is particularly relevant in studies investigating cellular protein degradation, signaling pathways, and disease mechanisms associated with proteasomal dysregulation. -
Calpain Inhibitor
A-933548 is a highly potent and selective inhibitor of calpain, demonstrating a Ki value of 18 nM. This compound's ability to modulate calpain activity makes it a valuable tool for research into neurodegenerative disorders, particularly Alzheimer's disease. Its specificity for calpain allows for detailed studies of calpain-mediated pathways and potential therapeutic interventions. -
Proteasomal Inhibitor
Z-Gly-Pro-Phe-Leu-CHO is a tetrapeptide aldehyde that serves as a highly selective and potent inhibitor of the proteasome. It demonstrates significant inhibition with Ki values of 1.5 µM for branched-chain amino acid-preferring activities, 2.3 µM for small neutral amino acid-preferring activities, and 40.5 µM for chymotrypsin-like activities, with an IC50 of 3.1 µM for peptidyl-glutamyl peptide hydrolyzing activity. This compound is valuable for research applications focusing on proteasomal functions and related pathways in cellular processes. -
Trypsin-like Proteasome Inhibitor
NC-002 is a cell-permeable trypsin-like proteasome inhibitor that selectively targets the proteasome while sparing lysosomal cysteine proteases. This epoxyketone derivative of Leupeptin enhances the sensitivity of myeloma cells to Bortezomib and Carfilzomib, making it a valuable tool for cancer research. NC-002's unique mechanism offers potential insights into proteasome-related pathways and therapeutic strategies in oncology. -
Proteasome Inhibitor
(+)-Catechin 3-gallate is a polyphenolic compound that functions as a non-selective proteasome inhibitor. It demonstrates antitumor activity by inducing apoptosis and decreasing the levels of inflammatory cytokines. This agent is of significant interest in cancer research, particularly for breast and prostate cancers, as well as in the study of neurodegenerative diseases such as Alzheimer's. -
Proteasome Inhibitor
Z-Leu-Leu-Tyr-COCHO is a potent proteasome inhibitor that specifically targets chymotrypsin-like activity, exhibiting a Ki value of 3.0 nM. This compound is effective in the modulation of protein degradation pathways, making it a valuable tool in studies related to cancer research and cellular stress responses. Its ability to inhibit proteasome activity provides insights into various biological processes and therapeutic mechanisms. -
Bortezomib Prodrug
Bortezomib-pinanediol is a prodrug of Bortezomib, functioning primarily as a proteasome inhibitor. This compound effectively inhibits cell growth and is utilized in research focused on multiple myeloma. Its ability to modulate proteasomal activity makes it a valuable tool for investigating cancer cell regulation and therapeutic responses. -
Proteasome Inhibitor
JBIR-22 is a proteasome inhibitor that specifically targets the homodimer of the proteasome assembly factor 3, disrupting its protein-protein interactions. This disruption leads to significant cytotoxic effects on human cervical cancer cell lines, demonstrating its potential as a therapeutic agent in oncology research. The stereochemical structure of JBIR-22 has been elucidated through total synthesis, supporting its further investigation in cancer studies. -
Proteasomal Substrate
MeOSuc-Gly-Leu-Phe-AMC is a peptide substrate specifically designed for proteasomal activity assays. This compound facilitates the study of proteasome function by serving as a sensitive probe for proteolytic activity. It is particularly useful in research areas focused on protein degradation pathways and cellular regulation mechanisms, providing insights into various biological processes and potential disease states. -
SAP2 Inhibitor
SAP2-IN-1 is a potent inhibitor of secreted aspartic protease 2 (SAP2), characterized by an IC50 value of 0.92 μM. This compound serves as a virulence factor inhibitor, making it valuable for studying the role of SAP2 in pathogenesis. Due to its unique mechanism, SAP2-IN-1 can be utilized in research focused on infectious diseases and the mechanisms of microbial virulence. -
β2/β2i-specific Active Probe
Az-NC-002 is a β2/β2i-specific active probe designed to selectively target the proteasome's trypsin-like site. This compound exhibits minimal off-target effects, demonstrating negligible inhibition of Cathepsin D, thus providing a highly specific tool for probing proteasome activity. Az-NC-002 is ideal for biochemical assays and research applications focused on proteasome function and regulation in various pathological conditions. -
Chymase Inhibitor
INVA8001 is a highly selective and orally active chymase inhibitor, demonstrating significant potency with IC50 values of 0.02 μM for human chymase and 0.03 μM for mouse mast cell proteinase 4 (mMCP-4). This compound exhibits remarkable selectivity over related serine proteases, with IC50 values of 3.4 μM for bovine α-chymotrypsin and 32.1 μM for human cathepsin G, showcasing over 1000-fold selectivity. INVA8001 has been shown to inhibit mast cell activity in a mouse model of primary sclerosing cholangitis (PSC), leading to improved bile duct pathology and reduced bile stasis, thus highlighting its potential anti-inflammatory and anti-fibrotic applications in research. -
Cage Xanthonoid
Isomoreollic acid is a cage xanthonoid that targets proteasome inhibition, exhibiting cytotoxic effects on colon cancer cells with an IC50 greater than 10 μM. Derived from the stem bark of Garcinia lateriflora, isomoreollic acid serves as a valuable reagent for colon cancer research, enabling studies on its mechanisms and potential therapeutic applications. -
LMP Inhibitor
LMP7/LMP2-IN-1 is a potent inhibitor of the immunoproteasome subunits LMP7 and LMP2, exhibiting IC50 values of 257 nM and 10 nM, respectively. This compound effectively reduces antibody production and downregulates B cells in the germinal centers of the spleen as well as plasma cells in NP-OVA-immunized mice. LMP7/LMP2-IN-1 is valuable for research into autoimmune diseases and the modulation of immune responses. -
Proteasome Inhibitor
Phepropeptin B is a proteasome inhibitor that demonstrates a potent inhibitory effect with an IC50 of 11 μg/mL. This microbial secondary metabolite plays a crucial role in the regulation of protein degradation, making it a valuable tool in studies related to cancer research and cellular processes involving proteostasis. Its application extends to exploring the mechanisms of diseases where proteasome activity is dysregulated. -
20S Proteasome Inhibitor
Cerpegin is a potent inhibitor of the 20S proteasome, which plays a critical role in the degradation of ubiquitinated proteins. This compound exhibits significant biological activities including anti-inflammatory, analgesic, and antiulcer effects, making it a valuable tool in research focused on proteasome-related pathways and therapeutic applications. Its mechanism of action allows for exploration in models of neuroprotection and various inflammatory conditions. -
Proteasome Inhibitor
Phepropeptin D is a microbial secondary metabolite that functions as a proteasome inhibitor, exhibiting an IC50 of 7.8 μg/mL. This compound plays a significant role in the regulation of protein degradation pathways, making it valuable for studies related to cellular proteostasis and cancer research. Its ability to modulate proteasome activity positions Phepropeptin D as a useful tool for investigating therapeutic strategies targeting proteasome-mediated pathways. -
Proteasome Control
Bortezomib impurity A is a metabolite of the 20S proteasome inhibitor Bortezomib, functioning as a key control for proteasome activity. This compound is useful in research applications focused on the mechanisms of proteasome inhibition and related signaling pathways. Its characterization aids in the development and quality assessment of proteasome-targeted therapeutics. -
HER2 Inhibitor
JBJ-08-178-01 is a selective tyrosine kinase inhibitor targeting mutant forms of the human epidermal growth factor receptor 2 (HER2). It demonstrates significant antitumor activity by reducing both the kinase activity and protein levels of HER2 through the induction of proteasomal degradation. This compound holds potential for research applications in non-small-cell lung cancer, providing insights into therapeutic mechanisms against HER2-driven malignancies. -
Proteasome Inhibitor
4-Nitrochalcone serves as a proteasome inhibitor, specifically targeting the proteasomal degradation pathway. It effectively inhibits the activity of NF-κB induced by TNFα, making it a valuable tool for studying inflammatory processes and signaling pathways. This compound is utilized in research focused on cancer, neurodegenerative diseases, and other conditions where proteasome activity plays a critical role. -
Antitumoral Agent
Argyrin A is a cyclical peptide that functions as a potent antitumoral agent through its ability to inhibit the proteasome. This inhibition results in increased levels of endogenous p27kip1 by blocking protein turnover, thereby contributing to its antitumor activity. Argyrin A is valuable for research applications focusing on cancer biology and therapeutic development targeting proteasomal pathways. -
Proteasome Inhibitor
Phepropeptin A is a microbial secondary metabolite that functions as a potent proteasome inhibitor, exhibiting an IC50 of 21 μg/mL. This compound is valuable for research applications focusing on the regulation of protein degradation pathways. Phepropeptin A can be utilized in studies aimed at understanding the role of proteasomal inhibition in cellular processes and disease models, particularly in cancer research and neurodegenerative disorders. -
Proteasome Inhibitor
Phepropeptin C is a proteasome inhibitor with a reported IC50 of 12.5 μg/mL. This microbial secondary metabolite disrupts protein degradation pathways, leading to the accumulation of regulatory proteins and altered cellular responses. Its ability to modulate proteasome activity makes it a valuable tool for research into cancer biology and other diseases characterized by dysregulated protein homeostasis. -
Chymase Inhibitor
BI-1942 is a potent chymase inhibitor with an IC50 of 0.4 nM for human chymase. This chemical probe is primarily utilized in research related to ophthalmic diseases, enabling the exploration of chymase's role in ocular pathologies. Its selective inhibition provides a valuable tool for investigating the therapeutic potential in conditions where chymase is implicated. -
Proteasome Inhibitor
RID-F (Ridaifen-F) is a nonpeptidic proteasome inhibitor that targets the human 20S proteasome. It demonstrates significant inhibitory activity with IC50 values of 0.64 µM for caspase-like (CT-L), 0.34 µM for trypsin-like (T-L), and 0.43 µM for post-glutamyl (PGPH) activities. RID-F is utilized in research focused on cellular degradation pathways, cancer biology, and therapeutic approaches targeting proteasome dysfunction. -
Proteasome Inhibitor
Chymase-IN-2 is a potent proteasome inhibitor that selectively modulates chymase activity. It exhibits significant efficacy in addressing inflammatory responses and disorders associated with serine protease activity. This compound is valuable for research aimed at understanding protease-mediated pathways and their implications in various diseases. -
Proteasome Inhibitor
Neurodegenerative Disorder-Targeting Compound 1 is a proteasome inhibitor that selectively targets calpain activity. This compound is designed to modulate cellular protein turnover, making it a valuable tool for studying the mechanisms of neurodegeneration. Its application spans various research areas, including the investigation of proteolytic pathways in neurodegenerative disorders and the exploration of therapeutic interventions aimed at enhancing neuronal survival. -
Fluorogenic Substrate
Ac-KQL-AMC is a fluorogenic substrate designed to quantify Trypsin-like activity. Upon cleavage by the proteasome, it produces a detectable fluorescence, making it a valuable tool for studying proteolytic activities in various biological contexts. This compound is particularly useful in research applications focused on protein degradation and turnover mechanisms. -
Trypsin Inhibitior
Nostosin G is a linear peptide that acts as a potent trypsin inhibitor, exhibiting an IC50 value of 0.1 μM. Comprised of three subunits—4-hydroxyphenyllactic acid, homotyrosine, and argininal—Nostosin G effectively modulates proteolytic activity. This compound is valuable for research applications focusing on digestive enzymes, protein processing, and potential therapeutic interventions in related disorders. -
Kallikrein Inhibitor
Kallikrein-IN-1 is a selective inhibitor of kallikrein enzymes. By modulating kallikrein activity, this compound plays a vital role in regulating various physiological processes including blood pressure and inflammation. It is valuable for research into cardiovascular diseases and potential therapeutic approaches targeting the kallikrein-kinin system. Kallikrein-IN-1's specificity makes it an important tool for studying enzymatic pathways and their implications in disease states. -
Protease Inhibitor
Dansyl-Glu-Gly-Arg-Chloromethylketone is a potent protease inhibitor that specifically targets serine/threonine proteases. Its mechanism involves the irreversible modification of the enzyme active site, effectively blocking protease activity. This compound is valuable for research applications focusing on blood coagulation processes and the role of serine proteases in various biological systems. Its use facilitates the study of proteolytic regulation mechanisms and contributes to the understanding of protease-targeted therapies. -
Trypsin Inhibitor
Bz-D-Arg-pNA hydrochloride is a competitive inhibitor of trypsin, a serine protease involved in protein digestion and regulation. This compound effectively modulates trypsin activity, making it a valuable tool for investigating protease functions and interactions in various biological systems. Its applications extend to studying enzyme kinetics and exploring the role of trypsin in physiological and pathological processes. -
Trypsin Substrate
Boc-QAR-pNA is a chromogenic substrate specifically designed for the detection of trypsin activity. Upon cleavage by trypsin, Boc-QAR-pNA releases a colored product, allowing for quantitative analysis of enzyme activity. This reagent is valuable in various research applications, including studies of proteolytic enzyme activity and screening for trypsin inhibitors. -
Tryptase Inhibitor
MOL-6131 is a highly selective, reversible inhibitor of tryptase, exhibiting a Ki value of 45 nM. This compound effectively reduces key features of allergic airway inflammation, including eosinophil infiltration in lung tissue, goblet cell hyperplasia, and mucus occlusion of airways. It serves as a valuable tool for research focused on respiratory diseases and allergic responses. -
FVII Inhibitor
Factor VII-IN-1 is a potent inhibitor of factor VII (FVII), exhibiting an IC50 of 1.1 μM. This compound demonstrates anticoagulant properties, making it a valuable tool for research applications focused on coagulation processes and thrombotic disorders. Factor VII-IN-1 can be utilized in studies aimed at understanding the mechanisms of blood coagulation and the development of anticoagulant therapies. -
Chymase Inhibitor
NK3201 is an orally active chymase inhibitor, demonstrating IC50 values of 2.5 nM, 1.2 nM, and 28 nM against human, dog, and hamster chymase, respectively. This compound effectively mitigates Bleomycin-induced pulmonary fibrosis and inhibits vascular proliferation in grafted veins. NK3201 serves as a valuable tool in research focused on fibroproliferative diseases and vascular complications. -
Protease Inhibitor
Leupeptin Ac-LL is a protease inhibitor derived from actinomycetes. It exhibits antiplasmin activity, making it useful in studies involving the regulation of proteolytic processes. This compound is commonly used in biochemical research to investigate protease functions and their roles in various biological pathways. -
DCLK1 inhibitor
DCLK1-IN-2 is a potent inhibitor of doublecortin-like kinase 1 (DCLK1) with an IC50 of 171.3 nM. This compound demonstrates significant antiproliferative activity against SW1990 cell lines, exhibiting an IC50 of 0.6 μM, and shows notable in vivo antitumor efficacy. DCLK1-IN-2 is suitable for research applications targeting DCLK1 in cancer biology and therapeutic development. -
Subtillsin Substrate
Fluorescent Substrate for Subtilisin is designed to specifically detect the enzymatic activity of subtilisin, a bacterial serine protease. This substrate provides a sensitive and quantifiable method to evaluate subtilisin activity in various biological assays. It is suitable for applications in enzyme activity studies and protease-related research. -
Trypsin-like Serine Protease Inhibitor
UAMC-00050 is a potent inhibitor of trypsin-like serine proteases. Its mechanism of action involves the selective blockade of these enzymes, which are implicated in various inflammatory processes. UAMC-00050 is particularly useful in research focused on dry eye syndrome and ocular inflammation, providing a valuable tool for elucidating the underlying mechanisms and potential therapeutic interventions in these conditions. -
Mast Cell Tryptase Inhibitor
APC 366 hydrochloride is a selective inhibitor of mast cell tryptase, specifically targeting its enzymatic activity. This compound effectively inhibits tryptase-induced histamine release in human tonsil and lung cells, highlighting its potential role in the modulation of allergic responses and inflammation. APC 366 hydrochloride is useful for research applications focusing on allergy-related mechanisms and inflammatory pathways. -
TPP II Inhibitor
Butabindide is a potent and selective inhibitor of tripeptidyl peptidase II (TPP II), exhibiting a Ki value of 7 nM for TPP II and a significantly higher Ki of 10 μM for TPP I. This compound effectively protects cholecystokinin-8 (CCK-8) from inactivation by inhibiting TPP II activity. Butabindide is valuable for research applications focused on TPP II-related pathways and the modulation of peptide activity in biological systems. -
Urinary Trypsin Inhibitor
Urinary Trypsin Inhibitor Fragment is a proteolytic fragment of urinary trypsin inhibitor that specifically targets protease activity. This fragment has been shown to inhibit tumor cell invasion, making it valuable for studies focused on cancer progression and metastasis. Its application extends to investigating the role of proteolytic regulation in various biological processes. -
Trypsin Inhibitor
Trypsin-IN-2 is a potent and highly selective inhibitor of human trypsin, exhibiting an IC₅₀ of 8 nM. This compound is valuable for studying the role of trypsin in various biological processes, particularly in the context of pancreatic cancer research. Its specificity and efficacy make it an important tool for elucidating the mechanisms underlying trypsin-related pathologies. -
WNK1 Inhibitor
Tyrphostin 47 is a potent inhibitor of WNK1, classified as a protein tyrosine kinase inhibitor. This compound effectively suppresses the proliferation of smooth muscle cells, making it a valuable tool for studying vascular biology and related pathologies. Tyrphostin 47 is utilized in various research applications focused on cellular signaling and growth regulation. -
Serine Proteinase Inhibitor
L 658758 is a potent inhibitor of serine proteinases, primarily targeting the active site of these enzymes. This compound exhibits strong biological activity, making it valuable for studies investigating proteolytic processes and related pathways. Research applications include elucidating the role of serine proteinases in various physiological and pathological conditions, as well as in drug discovery aimed at modulating these targets. -
Serine Protease
Complement factor D is a serine protease that plays a critical role in the complement system by activating C3 convertase through the specific cleavage of complement Factor B. This enzyme is essential for modulating immune responses and is promising for research in autoimmune diseases, such as paroxysmal nocturnal hemoglobinuria and C3 glomerulopathy, as well as conditions like age-related macular degeneration and thrombotic microangiopathies. Its study can provide insights into the underlying mechanisms of these diseases and potentially guide therapeutic development. -
cGKII Inhibitor
AP-C2 is a selective inhibitor of guanosine 3',5'-cyclic monophosphate-dependent protein kinase II (cGKII), exhibiting a pIC50 value of 5.2. This compound effectively modulates cGKII activity, making it a valuable tool in investigating cGMP signaling pathways. It is particularly relevant for research focused on cardiovascular biology and renal function, where cGKII plays a crucial role in cellular signaling. -
Chymotrypsin Substrate
Ac-Phe-Gly-pNA is a substrate specific for chymotrypsin, a serine protease. This compound undergoes enzymatic cleavage by chymotrypsin, resulting in the release of para-nitroaniline (pNA), which can be quantitatively measured, allowing for the assessment of enzyme activity. Ac-Phe-Gly-pNA is widely utilized in biochemical assays for studying chymotrypsin function and its kinetics in various biological research applications. -
Fluorogenic Substrate
Boc-Ala-Gly-Pro-Arg-AMC is a fluorogenic substrate designed for monitoring protease activity, particularly within serine proteases. This substrate is ideal for assessing enzymatic function in research applications involving protease activity, such as studying the oligopeptide enzyme B of Trypanosoma brucei. Its fluorescence allows for sensitive detection of enzymatic events, making it a valuable tool in biochemical and molecular biology studies.
