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Proteasome

Items 1-50 of 146

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Product Name
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  1. A11278
    PR-171 (Carfilzomib)

    Proteasome inhibitor

    PR-171 (Carfilzomib) is a tetrapeptide epoxyketone and a selective proteasome inhibitor. It is an analog of epoxomicin.
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  2. A12653
    ONX-0914

    Immunoproteasome inhibitor

    ONX 0914 is an immunoproteasome inhibitor with potential treatment applications in autoimmune disorders, such as rheumatoid arthritis, inflammatory bowel disease and lupus. ONX 0914 was designed to be a potent inhibitor of the immunoproteasome with minimal cross-reactivity for the constitutive proteasome.
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  3. A12768
    Lactacystin

    proteasome inhibitor

    Lactacystin is a cell-permeable, potent and selective proteasome inhibitor.
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  4. A12730
    Epoxomicin

    Proteasome inhibitor

    Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome.
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  5. A11043
    MG-132

    Proteasome inhibitor

    MG-132 is a potent cell-permeable inhibitor of proteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 μM).
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  6. A10160
    Bortezomib (Velcade)

    Proteasome inhibitor

    Bortezomib is a highly selective, reversible inhibitor of the 26S proteasome
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  7. A10600
    MLN2238 (Ixazomib)

    Proteasome Inhibitor

    MLN2238 is a potent reversible and specific β5 site of the 20S proteasome inhibitor with an IC50 value of 3.4 nM.
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  8. A13853
    Marizomib (NPI-0052, salinosporamide A)

    Proteasome Inhibitor

    Marizomib is a naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity.
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  9. A10602
    Ixazomib Citrate (MLN9708) Analogue

    Proteasome Inhibitor

    Ixazomib Citrate (MLN9708) Analogue is a proteasome inhibitor, which inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome.

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  10. A25350
    TP-110

    Proteasome Inhibitor

    TP-110 is a selective proteasome inhibitor that targets the protease-like activity of the 20S proteasome, leaving trypsin-like and peptidyl-glutamyl peptide hydrolysis activities unaffected. This compound effectively disrupts the NF-κB signaling pathway, leading to activation of caspases 3, 8, and 9, and subsequent PARP cleavage, while decreasing levels of anti-apoptotic proteins cIAP-1 and XIAP. TP-110 induces G2/M phase cell cycle arrest and promotes apoptosis in cancer cells, making it a valuable tool for researching various malignancies, including prostate cancer and multiple myeloma.
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  11. A31094
    Ub4ix

    Proteasome Inhibitor

    Ub4ix is a potent proteasome inhibitor that selectively protects K48-linked ubiquitin chains from deubiquitinating enzymes (DUBs), thereby preventing the degradation of ubiquitin-tagged proteins. This compound has demonstrated significant biological activity, including the reduction of cell viability and induction of apoptosis in HeLa cells, with an IC50 value of 1.6 μM. Ub4ix is a valuable tool for research applications focused on understanding protein homeostasis and the role of the proteasome in cellular processes.
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  12. A31646
    Baceridin

    Proteasome Inhibitor

    Baceridin is a proteasome inhibitor characterized as a cyclic hexapeptide. Isolated from the culture medium of Epiphytic Bacillus, it disrupts proteasome function, leading to inhibition of cell cycle progression and induction of apoptosis in tumor cells via a p53-independent mechanism. This compound is valuable for cancer research applications, particularly in studies exploring proteasome inhibition and its effects on tumor biology.
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  13. A26405
    AMC-3-030

    HDAC6/Proteasome Inhibitor

    AMC-3-030 is a selective inhibitor targeting histone deacetylase 6 (HDAC6) and the chymotrypsin-like activity of the proteasome, demonstrating IC50 values of 884 nM and 4.17 nM, respectively. This compound exhibits a proliferative inhibitory effect and has been shown to reduce levels of α-tubulin and β-actin. AMC-3-030 serves as a valuable tool for investigating mechanisms related to multiple myeloma and other related research applications.
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  14. A46016
    Apomorphine hydrochloride

    Dopamine receptor Agonist, 20S proteasome Activator

    Apomorphine hydrochloride is a potent dopamine receptor agonist and a known activator of the 20S proteasome. It enhances proteasomal and insulin-degrading enzyme activities, facilitating the degradation of intracellular amyloid-beta (Aβ), phosphorylated tau (p-tau), and p53, thereby reducing their levels in neuronal cells. This compound is particularly relevant for research focused on neurodegenerative disorders such as Alzheimer's disease and psychiatric conditions including schizophrenia.
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  15. A52314
    LXE408

    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).
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  16. A52330
    GNF6702

    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.
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  17. A52406
    GSK3494245

    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.
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  18. A52616
    Antitrypanosomal agent 15

    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.
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  19. A52632
    20S Proteasome-IN-4

    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.
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  20. A52838
    LXE408 fumarate

    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).
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  21. A52924
    Carmaphycin-17

    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.
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  22. A53014
    Proteasome-IN-8

    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.
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  23. A49196
    Argyrin B

    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.
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  24. A49416
    Octaarginine

    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.
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  25. A49723
    PR-39

    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.
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  26. A77294
    6-Chlorooxindole

    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.
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  27. A77296
    Vimentin-IN-1

    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.
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  28. A77297
    TCH-165

    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.
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  29. A77298
    20S Proteasome activator 1

    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.
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  30. A77299
    FiVe1

    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.
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  31. A77300
    Z-Ala-Arg-Arg-AMC

    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.
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  32. A77301
    PD 151746

    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.
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  33. A77302
    Zetomipzomib maleate

    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.
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  34. A77303
    Ac-PAL-AMC

    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.
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  35. A77304
    Alloxan hydrate

    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.
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  36. A77305
    NA-184

    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.
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  37. A77306
    MyoMed 205

    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.
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  38. A77307
    Ac-Nle-Pro-Nle-Asp-AMC

    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.
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  39. A77308
    Calpain-2-IN-1

    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.
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  40. A77309
    LU-005i

    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.
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  41. A77310
    5-Amino-8-hydroxyquinoline

    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.
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  42. A77311
    Boc3Arg

    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.
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  43. A77312
    Dazcapistat

    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.
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  44. A77313
    Zetomipzomib

    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.
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  45. A77314
    Ac-RLR-AMC

    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.
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  46. A77315
    LU-002i

    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.
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  47. A77316
    DPLG3

    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.
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  48. A77317
    BC-23

    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.
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  49. A77318
    Immunoproteasome activator 1

    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.
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  50. A77319
    Biotin-epoxomicin

    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.
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