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Catalog No.
Product Name
Application
Product Information
Citations
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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. -
Proteasome Inhibitor
Antitrypanosomal agent 15 is a selective proteasome inhibitor targeting Trypanosoma cruzi, with an impressive pIC50 of 7.4 for the T. cruzi proteasome and minimal activity (pIC50 < 4) against human proteasomes. This orally active compound demonstrates excellent brain penetration and favorable ADME properties, making it suitable for research focused on Chagas disease and related therapeutic interventions. Its selectivity and efficacy highlight its potential for advancing studies in trypanosomiasis. -
20S Proteasome Inhibitor
20S Proteasome-IN-4 is a selective inhibitor of the 20S proteasome, exhibiting an IC50 of 6.3 nM against Trypanosoma brucei brucei. This brain-penetrant compound is orally active and demonstrates potential for research into human African trypanosomiasis (HAT). Its specificity for the parasite makes it a valuable tool for studying proteasomal functions in this significant infectious disease. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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. -
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.
