Catalog No.
Product Name
Application
Product Information
Citations
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Proteasome Inhibitor
Enzyme-IN-1 is a potent proteasome inhibitor that targets the chymotrypsin-like activity (CT-L) of the 20S proteasome, specifically inhibiting N-terminal nucleophile (Ntn) hydrolases. This compound has demonstrated key biological activity in modulating protein degradation pathways, which may confer potential anti-inflammatory properties. Enzyme-IN-1 is suitable for research applications focused on studying proteasome-related processes and their implications in various disease models. -
20S Proteasome Inhibitor
20S Proteasome-IN-1 is a selective inhibitor of the 20S proteasome, functioning primarily by disrupting protein degradation pathways. This compound exhibits significant potential in studying various diseases, including cancer, immune-related disorders, inflammatory conditions, ischemic events, and neurodegenerative disorders. Its application in research enables a deeper understanding of proteasomal regulation and its role in cellular homeostasis and signaling pathways. -
Substrate
Calpain substrate is a fluorogenic substrate specifically designed for the assessment of calpain enzymatic activity. It is membrane non-permeable, ensuring precise measurement of calpain activity in biological samples. This reagent is suitable for applications in cellular signaling research and studies investigating calpain's role in various physiological and pathological processes. -
Proteasome Inhibitor
20S Proteasome-IN-2 is a selective inhibitor of the human 20S proteasome, specifically targeting the β5 subunit with an IC50 of 0.18 μM. This compound exhibits significant anti-proliferative effects in both in vitro and in vivo models, effectively inducing cell cycle arrest at the G2/M phase. It serves as a valuable tool for research focused on cancer biology and the mechanisms of proteasome function. -
RMCP I/RMCP II/Chymotrypsin Substrate
Suc-Ala-Ala-Pro-Phe-SBzl is a synthetic peptide substrate targeting rat intestinal mast cell proteases RMCP I and RMCP II, as well as chymotrypsin. It serves as a useful tool for investigating proteolytic activity in biochemical assays. Additionally, Suc-Ala-Ala-Pro-Phe-SBzl can be hydrolyzed by glycine (R208G), facilitating studies on enzyme specificity and catalytic mechanisms. This substrate is valuable in researching mast cell biology and protease functions. -
Proteasome-Activating Peptide
Proteasome-activating peptide 1 is a peptide that enhances chymotrypsin-like activity of the proteasome, thereby increasing proteolytic rates in vitro and in cellular cultures. This compound plays a significant role in preventing protein aggregation, demonstrated in cellular models of amyotrophic lateral sclerosis. Its ability to modulate proteasomal activity makes it a valuable tool for research into neurodegenerative diseases and protein homeostasis. -
Proteasome Inhibitor
RC-106 is a potent proteasome inhibitor, exhibiting an IC50 of 35 μM, and functions as a sigma receptor modulator. This compound demonstrates significant antiproliferative effects on various cancer cell lines, including glioblastoma and multiple myeloma. Its dual mechanism of action makes RC-106 a valuable reagent for research in cancer biology and therapeutic development. -
LMP7 Inhibitor
LMP7-IN-1 is a selective inhibitor targeting the immunoproteasome subunit LMP7 (β5i), with an IC50 of 1.83 nM. This boronic acid derivative demonstrates potent inhibition, making it an invaluable tool for research into protein degradation and immune response modulation. LMP7-IN-1 is applicable in studies focused on autoimmune diseases, cancer, and other conditions where immunoproteasome activity can impact cellular function and pathology. -
CD13 and Proteasome Inhibitors
BC-05 is a potent inhibitor of CD13 and the 20S proteasome, exhibiting an IC50 of 0.13 μM for human CD13 and 1.39 μM for the proteasome. This compound is orally active and serves as a valuable tool in the investigation of multiple myeloma and related hematological malignancies. Its dual-targeting mechanism makes BC-05 a significant reagent for elucidating pathways involved in cancer progression and therapeutic resistance. -
UPS Inhibitor
Leptosphaerodione is a potent inhibitor of the ubiquitin-proteasome system (UPS), isolated from the fungus Remotididymella sp. This compound exhibits significant cytotoxic effects in HeLa cells, with an IC50 value of 3.2 μM. Leptosphaerodione serves as a valuable tool for research applications related to cancer biology and the development of anti-tumor strategies. -
Proteasome Inhibitor
Tyropeptin A-4 is a potent proteasome inhibitor that specifically targets the mammalian 20S proteasome. It exerts its inhibitory effect by binding to the site responsible for trypsin-like activity, which is critical for protein degradation. This compound is valuable for research applications studying cellular processes involving proteasome activity and protein turnover, as well as potential therapeutic strategies for diseases related to proteasome dysfunction. -
Calpain-1 Inhibitor
Calpain Inhibitor XI is a reversible covalent inhibitor targeting calpain-1. This compound demonstrates significant inhibitory effects on calpain-1 activity, making it a valuable tool for studying neurodegenerative disorders and associated cellular pathways. Researchers can utilize Calpain Inhibitor XI to investigate the role of calpain-1 in various physiological and pathological processes. -
Proteasome Inhibitor
FV-162 is a potent, orally active, and irreversible proteasome inhibitor that demonstrates significant cytotoxicity in human myeloma cell lines and primary myeloma cells. This compound effectively inhibits tumor growth in myeloma xenograft mouse models, making it a valuable tool for cancer research. FV-162 is specifically applicable in the investigation of multiple myeloma and related therapeutic strategies. -
Calpain Inhibitor
AK 275 is a potent calpain inhibitor that demonstrates neuroprotective activity. Its mechanism of action involves the inhibition of calpain-mediated proteolysis, making it a valuable tool for investigating central nervous system trauma and ischemia. Researchers can utilize AK 275 to explore its therapeutic potential and underlying pathways in neurodegenerative conditions. -
Proteasome Inhibitor
Cadmium pyrithione is a metal compound that serves as a potent proteasome inhibitor, specifically targeting protein deubiquitinase activity. Its application leads to significant accumulation of ubiquitinated proteins in cancer and primary leukemia cells, contributing to its anticancer effects. By prominently inhibiting deubiquitinase activities, such as USP14 and UCHL5, Cadmium pyrithione induces apoptosis via caspase activation, while showing a lesser impact on 20S proteasome activity. Additionally, its suppression of proteasome function has been demonstrated to impede tumor growth in animal xenograft models, highlighting its potential for cancer research. -
19S RP Inhibitor
TCL1 is a selective non-covalent inhibitor that targets the Pru domain of the Rpn-13 subunit within the 19S regulatory particle (19S RP) of the proteasome, exhibiting an IC50 of approximately 26 μM. By disrupting the recognition and transport of ubiquitinated proteins, TCL1 inhibits proteasomal degradation, thereby influencing intracellular protein metabolism. This compound shows significant potential for studying hematological malignancies and related therapeutic strategies. -
Proteasome Inhibitor
ZINC09518833 is an α-ketoamide nonpeptidic proteasome inhibitor that demonstrates effective binding to both primed and nonprimed sites of the proteasome, with an IC50 value of 12.4 μM. This compound exhibits significant biological activity relevant to the treatment of multiple myeloma (MM), making it a valuable tool for research in cancer biology and therapeutic development. Its mechanism of action provides insights into proteasomal degradation pathways and their role in oncogenesis. -
LMP7 Inhibitor
LMP7-IN-2 is a selective inhibitor of the LMP7 protease, which is part of the immunoproteasome involved in antigen processing and inflammation regulation. This compound demonstrates significant biological activity in modulating inflammatory responses and has potential applications in the study of associated inflammatory diseases and disorders. Its use in research may aid in the understanding of immune mechanisms and the development of therapeutic strategies targeting inflammation. -
20S Proteasome Inhibitor
5-Amino-8-hydroxyquinoline dihydrochloride is a potent non-competitive inhibitor of the 20S proteasome. This compound effectively inhibits NF-κB activity, leading to apoptosis in cancer cells while exhibiting minimal cytotoxicity towards normal hematopoietic cells. Its unique properties make it a valuable tool for cancer research, particularly in studies related to leukemia and other malignancies. -
Proteasome Substrate
Z-Leu-Leu-Glu-βNA is a substrate specifically designed to assess the catalytic activity of glutamylpeptidyl-peptide hydrolase in the 20S proteasome. This fluorogenic substrate enables the monitoring of proteasome activity, which is crucial for studies involving protein degradation and regulation in various cellular processes. Researchers can utilize Z-Leu-Leu-Glu-βNA in assays that explore the role of the proteasome in pathophysiological conditions and drug responses. -
20S Proteasome Inhibitor
20S Proteasome-IN-3 is a potent inhibitor of the 20S proteasome β5 subunit, with an IC50 value of 1.64 μM. This compound exhibits significant anti-tumor proliferation activity, making it a valuable tool in cancer research. It is useful for studies investigating the role of proteasome inhibition in tumor biology and therapeutic applications. -
Proteasome Inhibitor
Proteasome β2c/i-IN-1 is a selective inhibitor of the human proteasome subunits β2c and β2i. This compound effectively impairs proteasome function, leading to the accumulation of ubiquitinated proteins. It is utilized in research applications focused on protein degradation pathways, cellular stress responses, and mechanisms of cancer development. -
Proteasome Inhibitor
Z-LLF-CHO (Z-Leu-Leu-Phe-CHO) is a potent inhibitor of the chymotrypsin-like activity of the proteasome, exhibiting an inhibition constant (Ki) of 460 nM. This compound also functions as an inhibitor of NF-κB nuclear translocation, making it valuable for studies involving immune response and inflammation. Research applications include investigations into proteolytic processes and the role of cytokines in various disease models. -
Proteasome Inhibitor
TIR-199 is a selective dual proteasome inhibitor targeting the PSMB5 subunit of the constitutive proteasome and the PSMB8 subunit of the immunoproteasome. This compound exhibits significant cytotoxicity against various tumor cell lines, making it a valuable tool for cancer research. TIR-199 is particularly relevant for studies focused on multiple myeloma and the underlying mechanisms of proteasome inhibition in neoplastic cell death. -
Proteasome Inhibitor
Davelizomib is a potent proteasome inhibitor that exerts antineoplastic effects through the disruption of protein degradation pathways. By inhibiting the proteasome, it promotes the accumulation of pro-apoptotic factors and enhances the apoptotic response in cancer cells. This compound is primarily utilized in cancer research to explore therapeutic strategies against multiple myeloma and other malignancies. -
proteasome Inhibitor
Proteasome-IN-5 is a selective proteasome inhibitor that disrupts the ubiquitin-proteasome pathway, leading to the accumulation of polyubiquitinated proteins. This compound exhibits significant antitumor activity and is valuable in research related to cancer biology and neurodegenerative diseases. Proteasome-IN-5 can be utilized to study the role of proteasomal degradation in cellular processes and to explore potential therapeutic strategies targeting proteasome dysfunction. -
LMP2 Inhibitor
LU-001i is a selective inhibitor of the proteasome β1i subunit (LMP2). While LU-001i exhibits minimal immunomodulatory effects as a standalone treatment, its combination with LMP7 inhibitors, such as PRN1126, enhances anti-inflammatory and immunomodulatory activities. This reagent is valuable for investigating the mechanisms underlying autoimmune diseases and developing targeted therapeutic strategies. -
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.
