Proteasome

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  1. Proteasome inhibitor

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

    Lactacystin is a cell-permeable, potent and selective proteasome inhibitor.
  4. 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.
  5. Proteasome inhibitor

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

    Bortezomib is a highly selective, reversible inhibitor of the 26S proteasome
  7. Proteasome Inhibitor

    MLN2238 is a potent reversible and specific β5 site of the 20S proteasome inhibitor with an IC50 value of 3.4 nM.
  8. Proteasome Inhibitor

    Marizomib is a naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity.
  9. 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.

  10. 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.
  11. 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.
  12. 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.
  13. 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.
  14. 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.
  15. 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).
  16. 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.
  17. 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.
  18. 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.
  19. 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.
  20. 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.
  21. 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.
  22. 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).
  23. 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.
  24. 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.
  25. 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.
  26. Proteasome inhibitor

    CEP-18770 is a novel orally active proteasome inhibitor with a favorable tumor selectivity profile for the treatment of MM and other malignancies responsive to proteasome inhibition.
  27. Reversible Proteasome Inhibitor

    MG-115 is a potent, reversible peptide aldehyde inhibitor of proteasome chymotrypsin-like and caspase-like activities. It induces p53 dependent apoptosis.
  28. NF-kB inhibitor/Proteasome activator

    18α-Glycyrrhetinic acid (18α-GA) is a bioactive triterpenoid found in licorice. It shows selective inhibition of 11-HSD1 (11-hydroxysteroid dehydrogenase 1).
  29. Proteasome inhibitor

    MG-262, a boronic peptide acid, is a potent proteasome inhibitor that selectively and reversibly inhibits the chymotryptic activity of the proteasome.
  30. proteasome inhibitor

    Proteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1.
  31. Proteasome inhibitor

    RA190, a bis-benzylidine piperidon, inhibits proteasome function by covalently binding to cysteine 88 of ubiquitin receptor RPN13.
  32. Proteasome inhibitor?€?

    VR23 is a small molecule that potently inhibited the activities of trypsin-like proteasomes (IC50 = 1 nM), chymotrypsin-like proteasomes (IC50 = 50-100 nM), and caspase-like proteasomes (IC50 = 3uM).
  33. 20S proteasome inhibitor

    Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains of Aspergillus and other fungi.
  34. PSI

    Proteasome inhibitor

    PSI is a proteasome inhibitor that inhibits chymotrypsin-like activity of the proteasome.
  35. reversible proteasome inhibitor

    PI-1840 is a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity.
  36. Proteasome inhibitor

    ONX 0912 is a tripeptide epoxyketone, which inhibits growth and induces apoptosis in MM cells resistant to conventional and bortezomib therapies.
  37. 20S proteasome inhibitor

    Ixazomib citrate (MLN9708) is a reversible inhibitor of the chymotrypsin-like proteolytic β5 site of the 20S proteasome with an IC50 of 3.4 nM and a Ki of 0.93 nM.
  38. proteasome inhibitor

    (R)-MG-132 ((S,R,S)-(-)-MG-132) is the enantiomer of MG-132. (R)-MG-132 is a proteasome inhibitor with weaker cell cytotoxicity than MG-132. (R)-MG-132 stereoisomer is a more potent proteasome inhibitor than MG-132.
  39. DD1

    proteasome inhibitor

    DD1 is a proteasome inhibitor that induces human myeloid tumor-selective apoptosis.
  40. Tomatine is an glycoalkaloid that occurs in the extract of leaves of wild tomato plants. It has been found to inhibit the growth of various fungi and bacteria. It is used as a precipitating agent for steroids.
  41. proteasome-associated deubiquitinating enzymes inhibitor

    RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity.
  42. chymotrypsin inhibitor

    FK-448 Free base is an effective and specific inhibitor of chymotrypsin, with an IC50 of 720 nM.
  43. proteasome isopeptidase Rpn11 inhibitor

    Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.
  44. LMP7 inhibitor

    M3258 is an inhibitor of immunoproteasome (LMP7), may used in the research of inflammatory and autoimmune diseases, neurodegenerative diseases, proliferative diseases and cancer.

  45. HDAC/proteasome inhibitor

    RTS-V5 is a dual HDAC/proteasome inhibitor with IC50s of 6.9, 18, 15, 0.27, 0.53 μM for HDAC1, HDAC2, HDAC3, HDAC6, HDAC8, respectively.
  46. proteasome subunit Rpn11 inhibitor

    Rpn11-IN-1 (Capzimin intermediate) is a potent and selective inhibitor of proteasome subunit Rpn11 with an IC50 of 390 nM.
  47. proteasome β1i (LMP2) subunit inhibitor

    ML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor.
  48. LMP2 inhibitor

    KZR-504 is a highly selective inhibitor of immunoproteasome low molecular mass polypeptide 2 (LMP2), with IC50s of 51 nM, 4.274 μM for LMP2 and LMP7, respectively. KZR-504 is of interest for the treatment of autoimmune disease.
  49. alpains 1 and 2 inhibitor

    Alicapistat (ABT-957) is an orally active selective inhibitor of human calpains 1 and 2 for the potential use in the treatment of Alzheimer's disease (AD).
  50. 20S proteasome inhibitor

    Aclarubicin A, an anthracycline drug, specific inhibitor of the 20S proteasome chymotrypsin-like activity.

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