Proteasome

Catalog No.Inhibitor Name Proteasome20S proteasome
A10160Bortezomib (PS-341)
****
A11043MG-132
*
A11278Carfilzomib (PR-171)
***
A10602MLN9708
***
A10600Ixazomib (MLN2238)
****
A12653ONX-0914 (PR-957)
**
A14181Oprozomib (ONX 0912)
**
A11145Delanzomib (CEP-18770)
***
A10192Celastrol
*
A13650VR23
****
A14146PI-1840
**
A12730Epoxomicin

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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  1. VR23

    Catalog No. A13650
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    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). Learn More
  2. Epoxomicin

    Catalog No. A12730
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    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. Learn More
  3. AM 114

    Catalog No. A14922
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    20S proteasome inhibitor
    AM 114, a derivative of boronic chalcone, is a potent small-molecule inhibitor of the proteasome that inhibits the chymotrypsin-like activity of the 20S proteasome, with a value of 50% inhibition concentration IC50 of approximately 1 uM, resulting in a significant accumulation of ubiquitinated p53 and other cellular proteins in whole cells without significantly disrupting the interaction of p53 and murine double minute 2 (mdm2) proteins. Learn More
  4. MLN9708

    Catalog No. A10602
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    Proteasome Inhibitor
    MLN9708 is a proteasome inhibitor, which inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome. Learn More
  5. Proteasome Inhibitor
    Marizomib is a naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity. Learn More
  6. Aclacinomycin A

    Catalog No. A14910
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    20S proteasome inhibitor
    Aclarubicin A, an anthracycline drug, specific inhibitor of the 20S proteasome chymotrypsin-like activity. Learn More
  7. Dihydroeponemycin

    Catalog No. A14932
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    Proteasome inhibitor
    Dihydroeponemycin is an inhibitor of proteasome and antitumor reagent. Learn More
  8. Clasto-Lactacystin b-lactone

    Catalog No. A15427
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    20S proteasome inhibitor
    Clasto-lactacystin b-lactone was later identified as the active metabolite of lactacystin, resulting from the elimination of cysteine and the formation of a reactive b-lactone. Learn More
  9. MG-115

    Catalog No. A11601
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    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. Learn More
  10. PI-1840

    Catalog No. A14146
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    reversible proteasome inhibitor
    PI-1840 is a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity. Learn More
  11. ONX 0912 (Oprozomib)

    Catalog No. A14181
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    Proteasome inhibitor
    ONX 0912 is a tripeptide epoxyketone, which inhibits growth and induces apoptosis in MM cells resistant to conventional and bortezomib therapies. Learn More
  12. PSI

    Catalog No. A14048
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    Proteasome inhibitor
    PSI is a proteasome inhibitor that inhibits chymotrypsin-like activity of the proteasome. Learn More
  13. Bortezomib (Velcade)

    Catalog No. A10160
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    Proteasome inhibitor
    Bortezomib is a highly selective, reversible inhibitor of the 26S proteasome Learn More
  14. MG-132

    Catalog No. A11043
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    Proteasome inhibitor
    MG-132 is a potent cell-permeable inhibitor of proteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 μM). Learn More
  15. MLN2238 (Ixazomib)

    Catalog No. A10600
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    Proteasome Inhibitor
    MLN2238 is a potent reversible and specific β5 site of the 20S proteasome inhibitor with an IC50 value of 3.4 nM. Learn More
  16. CEP-18770 (Delanzomib)

    Catalog No. A11145
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    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. Learn More
  17. PR-171 (Carfilzomib)

    Catalog No. A11278
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    Proteasome inhibitor
    PR-171 (Carfilzomib) is a tetrapeptide epoxyketone and a selective proteasome inhibitor. It is an analog of epoxomicin. Learn More
  18. ONX-0914

    Catalog No. A12653
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    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. Learn More
  19. Lactacystin

    Catalog No. A12768
    proteasome inhibitor
    Lactacystin is a cell-permeable, potent and selective proteasome inhibitor. Learn More
  20. Gliotoxin

    Catalog No. A13711
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    20S proteasome inhibitor
    Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains of Aspergillus and other fungi. Learn More
  21. MG-262

    Catalog No. A12220
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    Proteasome inhibitor
    MG-262, a boronic peptide acid, is a potent proteasome inhibitor that selectively and reversibly inhibits the chymotryptic activity of the proteasome. Learn More

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