Catalog No.
Product Name
Application
Product Information
Citations
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Proteasome Inhibitor
LXE408 fumarate is a non-competitive proteasome inhibitor selectively targeting kinetoplastids. It exhibits potent inhibitory activity with an IC50 of 0.04 μM against the L. donovani proteasome, demonstrating an EC50 of 0.04 μM for L. donovani itself. With limited ability to penetrate the blood-brain barrier, LXE408 fumarate is primarily suitable for research in visceral leishmaniasis (VL). -
Proteasome Inhibitor
Carmaphycin-17 is a selective 20S proteasome inhibitor, with an EC50 value of 217 nM. This compound exhibits strong antimicrobial activity against Trichomonas vaginalis, effectively overcoming Metronidazole resistance. It significantly reduces parasite burden in a topical treatment model without noted adverse effects. Carmaphycin-17 is a valuable tool for research on sexually transmitted diseases, specifically trichomoniasis. -
Pf Proteasome Inhibitor
Proteasome-IN-8 is a specific inhibitor of the proteasome in Plasmodium falciparum. This compound demonstrates notable antiparasitic activity against the P. falciparum 3D7 strain. It is a valuable tool for research into the mechanisms of malaria pathogenesis and the development of therapeutic strategies targeting parasitic proteasomes. -
Proteasome Inhibitor
LXE408 is an orally active, non-competitive inhibitor of the proteasome, exhibiting selective action against kinetoplastids. With an IC50 of 0.04 μM for the L. donovani proteasome, LXE408 effectively inhibits parasite proliferation, demonstrated by an EC50 of 0.04 μM against L. donovani. Due to its limited ability to cross the blood-brain barrier, LXE408 is particularly suitable for research focused on visceral leishmaniasis (VL). -
Kinetoplastid Proteasome Inhibitor
GNF6702 is a selective inhibitor of the kinetoplastid proteasome, targeting the degradation pathway critical for parasite survival. This compound demonstrates potent activity against various kinetoplastid parasites and has shown efficacy in clearing infections in murine models of leishmaniasis, Chagas disease, and human African trypanosomiasis. GNF6702 is valuable for research focused on developing therapies for these neglected tropical diseases. -
L. donovani Proteasome Inhibitor
GSK3494245 is a selective inhibitor of the chymotrypsin-like activity of the Leishmania donovani proteasome, targeting a site between the β4 and β5 subunits with an IC50 of 0.16 μM. This compound demonstrates moderate inhibitory effects on the chymotrypsin-like activity of human proteasomes, exhibiting IC50 values of 13 µM in purified 26S and 40 µM in enriched THP-1 extracts. GSK3494245's potent activity and favorable biosafety profile make it a valuable tool for research in parasitology and potential therapeutic applications against leishmaniasis. -
Immunoproteasome Inhibitor
Argyrin B is a natural cyclic peptide that functions as a reversible, non-competitive inhibitor of the immunoproteasome. It demonstrates selective inhibition of the β5i and β1i subunits, with a nearly 20-fold preference for β1i over the corresponding β1c subunit found in the constitutive proteasome. In addition to its role in proteasome inhibition, Argyrin B exhibits significant antibacterial properties, making it valuable for research in immunology and antimicrobial studies. -
Cell-penetrating Peptide/Proteasome Inhibitor
Octaarginine is a cell-penetrating peptide and potent proteasome inhibitor. It exhibits mixed-type inhibition against the chymotrypsin-like, caspase-like, and trypsin-like activities of the 20S proteasome while displaying reduced efficacy against the 26S proteasome. This compound facilitates the accumulation of ubiquitin-conjugated proteins and promotes HSPG-dependent cellular internalization through macropinocytosis, thereby enhancing the uptake of liposomal cargo and gene delivery. Octaarginine is valuable for research related to cervix carcinoma, collagen antibody-induced arthritis, and bacterial infections. -
Proteasome Inhibitor
PR-39 is a natural proline- and arginine-rich antibacterial peptide that functions as a noncompetitive, reversible allosteric inhibitor of the proteasome. By binding to the α7 subunit of the proteasome, PR-39 effectively blocks the degradation of NF-κB inhibitor IκBα through the ubiquitin-proteasome pathway. This compound demonstrates key biological activities such as stimulating angiogenesis and inhibiting inflammatory responses, making it a valuable tool for research on myocardial infarction and inflammatory diseases. -
Chymase Inhibitor
6-Chlorooxindole is a selective chymase inhibitor, exhibiting an IC50 of 470 μM. This compound demonstrates over 100-fold selectivity for chymase compared to cathepsin G. 6-Chlorooxindole is valuable for research applications focused on cardiovascular disease mechanisms and therapeutic interventions. -
Vimentin Inhibitor
Vimentin-IN-1 is a selective vimentin inhibitor that acts by binding to the type III intermediate filament protein, vimentin (VIM). This binding induces hyperphosphorylation at Ser56, leading to the selective disruption of mitosis and consequent multinucleation in vimentin-expressing mesenchymal cancer cells. Vimentin-IN-1 demonstrates improved oral bioavailability and favorable pharmacokinetic properties compared to its precursor, FiVe1, making it a valuable tool for cancer research applications focused on targeting vimentin-related pathways. -
Proteasome Assembly Modulator
TCH-165 is a small molecule proteasome assembly modulator that enhances the levels of the 20S proteasome. This compound facilitates 20S-mediated protein degradation, making it a valuable tool for studying protein turnover and homeostasis. TCH-165 is applicable in research involving cancer biology, neurodegenerative diseases, and cellular stress responses. -
20S Proteasome Activator
20S Proteasome Activator 1 is a potent activator of the 20S proteasome, demonstrating effective EC200 values of 0.3 μM, 0.7 μM, and 1.8 μM for trypsin-like, chymotrypsin-like, and caspase-like activities, respectively. This compound functions effectively within cellular environments, mitigating the accumulation of the pathogenic A53T mutant of α-synuclein. It is particularly useful for research in the context of neurodegenerative diseases, facilitating studies on proteostasis and related therapeutic approaches. -
Vimentin Inhibitor
FiVe1 is a potent inhibitor of vimentin (VIM), targeting its rod domain to induce disassembly and hyperphosphorylation at Ser56. This mechanism results in mitotic catastrophe, multinucleation, and a loss of stemness in cancer cells. FiVe1 demonstrates anticancer effects, particularly against soft tissue sarcomas, and enhances the sensitivity of ovarian cancer cells to Cisplatin. This compound is valuable for research involving mesenchymal cancers, such as breast cancer and soft tissue sarcoma, as well as ovarian cancers. -
Proteasome Substrate
Z-Ala-Arg-Arg-AMC is a fluorogenic proteasome substrate designed to specifically assay the trypsin-like activity of the proteasome. Its unique structure allows for sensitive detection of proteolytic activity, making it a valuable tool for studying protein degradation and turnover in cellular processes. This substrate is widely utilized in research applications focused on proteasome function and its implications in various diseases. -
Calpain Inhibitor
PD 151746 is a potent calpain inhibitor that demonstrates 20-fold selectivity for u-calpain, with a reported inhibition constant (Ki). This compound is primarily utilized in research to study the role of calpain in various biological processes, including calcium-regulated proteolysis and cellular signaling pathways. Its effectiveness makes it a valuable tool for investigating calpain's contribution to diseases such as neurodegeneration and cardiac dysfunction. -
Immunoproteasome Inhibitor
Zetomipzomib maleate is a first-in-class immunoproteasome inhibitor that selectively targets the LMP7 and LMP2 subunits, demonstrating IC50 values of 39 nM and 131 nM, respectively. This compound is primarily utilized in the study of autoimmune diseases, where it may modulate immune responses by inhibiting immunoproteasome activity. Its distinct mechanism offers a valuable tool for researchers investigating the pathological roles of the immunoproteasome in various disorders. -
LMP2 Fluorogenic Substrate
Ac-PAL-AMC is a fluorogenic substrate specifically designed for the 20S proteasome LMP2/β1i activity. It is utilized in biochemical assays to monitor proteasomal degradation processes, facilitating research into protein turnover and associated cellular functions. This substrate can enable real-time measurement of protease activity, making it an essential tool for studies in cancer, neurodegeneration, and other diseases linked to proteostasis. -
Diabetogenic Agent/Proteasome Inhibitor
Alloxan hydrate is a diabetogenic agent that induces diabetes by selectively destroying insulin-secreting beta cells in the pancreas. Additionally, it acts as a proteasome inhibitor, disrupting protein degradation pathways. This compound is widely utilized in research to study diabetes mechanisms and the role of proteasome activity in cellular processes. -
Calpain-2 Inhibitor
NA-184 is a selective calpain-2 inhibitor, demonstrating an IC50 of 134 nM against mouse calpain-2, with minimal activity towards calpain-1 (IC50 of 2826 nM). This compound exhibits significant neuroprotective properties, making it a valuable tool for research on traumatic brain injury (TBI). Additionally, NA-184 shows limited inhibition of other protease classes, underscoring its specificity in experimental settings. -
MuRF1 Inhibitor
MyoMed 205 is a potent MuRF1 inhibitor that functions by preventing the ubiquitination and proteasomal degradation of skeletal muscle proteins. This compound enhances muscle performance and mitigates muscle wasting and weight loss associated with various conditions. MyoMed 205 is suitable for research applications related to cancer cachexia, type 2 diabetes mellitus, and heart failure with preserved ejection fraction, making it a valuable tool in understanding muscle atrophy and metabolic disorders. -
26S Proteasome Substrate
Ac-Nle-Pro-Nle-Asp-AMC is a specific substrate designed for the 26S proteasome, targeting its catalytic activities. This compound is utilized primarily for assessing the caspase-like activity of the 26S proteasome in various biological studies. Its application is crucial for understanding proteasomal regulation and function in cellular processes. -
Calpain-2 Inhibitor
Calpain-2-IN-1 is an isoform-specific inhibitor targeting calpain-2, exhibiting a Ki of 7.8 nM for calpain-2 and 181 nM for calpain-1. This selective inhibition allows for precise modulation of calpain-2 activity, making it a valuable tool in the study of neurodegenerative diseases and disorders affecting synaptic function. Its application in research provides insights into the role of calpain-2 in various cellular processes and disease mechanisms. -
Immunoproteasomes Inhibitor
LU-005i is a potent inhibitor of the β5i subunit of immunoproteasomes, demonstrating an IC50 of 6.6 nM and selectivity over the β5c subunit with an IC50 of 287 nM. This compound is valuable for research into modulation of immune responses and antigen processing, offering insights into autoimmune diseases and cancer immunotherapy. Its specificity for immunoproteasomes makes it a useful tool for studying the role of proteasomal pathways in various biological processes. -
20S Proteasome Inhibitor
5-Amino-8-hydroxyquinoline is a non-competitive inhibitor of the 20S proteasome, demonstrating potent inhibitory effects on NF-κB activity. This compound induces apoptosis in cancer cells while exhibiting minimal cytotoxicity towards normal hematopoietic cells. It is valuable for research applications in cancer biology, particularly in the study of leukemia and related malignancies. -
Arg Tag
Boc3Arg is a tert-butyl carbamate-protected form of arginine, designed to facilitate protein degradation by targeting the 20S proteasome. Its unique properties enable efficient localization of tagged proteins for proteasomal degradation, making it a valuable tool in studies of protein turnover and regulation. Boc3Arg is particularly useful in research applications that investigate ubiquitin-proteasome pathways and protein quality control mechanisms in cells. -
Calpain Inhibitor
Dazcapistat is an orally active small-molecule inhibitor targeting calpain 1, 2, and 9. This compound significantly reduces the expression and production levels of IL-6 in injured lung tissue, contributing to decreased fibrosis. Dazcapistat exhibits anti-fibrotic properties in various animal models, including those for skin, liver, and lung fibrosis. Its applications extend to research on coronavirus disease 2019 (COVID-19) and idiopathic pulmonary fibrosis. -
Immunoproteasome Inhibitor
Zetomipzomib is a selective inhibitor of the immunoproteasome, specifically targeting the LMP7 and LMP2 subunits with reported IC50 values of 39 nM and 131 nM, respectively. This first-in-class compound demonstrates significant potential in the investigation of autoimmune diseases, providing a valuable tool for research into the modulation of immune responses and proteasomal degradation pathways. Researchers can utilize Zetomipzomib to explore therapeutic avenues for conditions where the immunoproteasome plays a critical role. -
26S Proteasome Substrate
Ac-RLR-AMC is a fluorogenic substrate specifically designed for the 26S proteasome pathway. Upon proteolytic cleavage, the release of 7-amino-4-methylcoumarin (AMC) generates fluorescence, facilitating the quantification of trypsin-like activity within the proteasome. This reagent is valuable for research applications focused on proteasome function, cellular regulation, and related biochemical assays. -
Proteasome Inhibitor
LU-002i is a selective inhibitor of the β2c and β2i subunits of the human proteasome, exhibiting an IC50 of 220 nM for the β2i subunit. This compound is valuable for research applications involving protein degradation and cellular stress responses. Its specific targeting can aid in the elucidation of proteasome-related pathways and the development of therapeutic strategies for conditions influenced by proteasome activity. -
Immunoproteasome β5i Subunit Inhibitor
DPLG3 is a selective inhibitor of the immunoproteasome β5i subunit, demonstrating an IC50 of 4.5 nM. It effectively inhibits the mouse i-20S proteasome with an IC50 value of 9.4 nM. DPLG3 is capable of downregulating the protein levels of NF-κB p50 and p65, highlighting its potential in the study of immune-related diseases and therapeutic applications. -
Proteasome Inhibitor
BC-23 (NSC 45382) is a potent proteasome inhibitor that selectively inhibits the chymotrypsin-like (CT-L) activity of the proteasome complex. This compound demonstrates significant cytotoxicity against malignant cells while sparing normal cells, making it a valuable tool for cancer research. BC-23 is utilized in studies aimed at elucidating the role of proteasomal degradation in cell cycle regulation and tumor progression. -
Immunoproteasome Activator
Immunoproteasome Activator 1 is a selective activator of the immunoproteasome that enhances the presentation of MHC-I-bound peptides by over 100-fold. This compound functions by binding to the proteasome structural subunit PSMA1, facilitating the association of the proteasome activator PA28α/β (PSME1/PSME2) with immunoproteasomes. Its significant biological activity makes it valuable for research focused on immune response modulation and antigen processing. -
Proteasome Subunit Binder
Biotin-epoxomicin is a proteasome subunit binder that serves as an affinity reagent for the identification and purification of proteasomal catalytic subunits. This compound enables the affinity purification of active subunits, facilitating their subsequent analysis via liquid chromatography-mass spectrometry (LC-MS). Biotin-epoxomicin is particularly useful in research applications focused on solid tumors, such as those derived from B16 melanoma, providing insights into proteasome function in cancer biology. -
calpain I Inhibitor
(Rac)-Calpain Inhibitor XII is a reversible and selective inhibitor of calpain I, exhibiting a binding affinity of Ki=19 nM. This compound displays reduced binding to calpain II (Ki=120 nM) and cathepsin B (Ki=750 nM), making it a valuable tool for dissecting calpain-related biochemical pathways. Its applications span various fields, including studies on neutrophil chemotaxis, neuronal signaling, and cardiac responses to injury, facilitating insights into calpain's role in cellular processes and pathologies. -
20S Proteasome Substrate
Z-Leu-Leu-Leu-AMC is a fluorogenic substrate designed for the assessment of chymotrypsin-like protease activity in the 20S proteasome. It provides a sensitive and specific means to monitor proteasomal function and proteolytic activity. This reagent is valuable for research applications involving protein degradation, cellular homeostasis, and the study of proteasome-related diseases. -
Proteasome Inhibitor
Biotin-(Oaa)3-epoxomicin is a biotinylated proteasome inhibitor derived from Epoxomicin, connected through three hydrophilic oxaacetyl amino acid linkers. This compound is utilized primarily in proteomic research for the capture and identification of proteasome complexes, facilitating target validation and elucidation of intracellular targets. Epoxomicin effectively inhibits proteasome activity through covalent binding to catalytic subunits such as LMP7, X, MECL1, and Z, with a pronounced effect on chymotrypsin-like activity, while sparing non-proteasomal proteases like trypsin and papain. Additionally, it serves as an NF-κB inhibitor, demonstrating potential in studies of inflammatory responses. -
Immunoproteasome/Proteasome Inhibitor
Immunoproteasome inhibitor 1 is a potent reversible inhibitor of the immunoproteasome and the proteasome, targeting the β5c, β1i, and β5i subunits with Kis of 1.18, 0.27, and 1.91 μM, respectively. This compound exhibits significant biological activity in modulating protein degradation pathways, making it a valuable tool for investigating the role of the immunoproteasome in various neoplastic diseases. Its unique mechanism of action facilitates research into targeted therapies and mechanistic studies in oncology. -
Calpain Inhibitor
Ac-Leu-Leu-Norleucinol (ALLN) is a potent calpain inhibitor that plays a critical role in the study of proteolytic pathways. This compound has demonstrated effectiveness in mitigating acetaminophen-induced acute liver damage by lowering the levels of liver enzymes such as alanine aminotransferase (ALT) and aspartate aminotransferase (AST). Its application extends to research focused on cellular stress responses and the mechanisms of liver injury. -
Ubiquitin-proteasome System Stressor
RAMB4 is a potent ubiquitin-proteasome system (UPS) stressor that inhibits ubiquitin-mediated protein degradation upstream of the 20S proteasomal catalytic activities. By triggering a UPS-stress response, RAMB4 effectively disrupts protein homeostasis without directly impacting the catalytic functions of the 20S proteasome. Its unique mechanism positions RAMB4 as a valuable tool for investigating UPS-related pathways and contributes to anticancer research by enhancing cellular stress responses. -
Calpain Inhibitor
(1S,2R)-Alicapistat is a selective inhibitor of human calpains 1 and 2, targeting these proteolytic enzymes involved in cellular signaling. With an IC50 value of 395 nM for calpain 1, it demonstrates significant biological activity, potentially making it valuable in Alzheimer's disease research. This compound's oral bioavailability and specificity may aid in elucidating the role of calpains in neurodegenerative disorders. -
Calpain 1 Inhibitor
Calpain Inhibitor-1 is a selective inhibitor of calpain 1, a cysteine protease, with an IC50 value of 100 nM and a Ki of 2.89 μM. This compound is instrumental in studying calpain-mediated processes, including cellular signaling and apoptosis. It serves as a valuable tool in research applications focusing on neurodegenerative diseases, cardiac protection, and cancer therapy, where calpain activity is implicated. -
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.
