Proteasome
Catalog No. | Inhibitor Name | Proteasome | 20S proteasome |
---|---|---|---|
A10160 | Bortezomib (PS-341) | **** | |
A11043 | MG-132 | * | |
A11278 | Carfilzomib (PR-171) | *** | |
A10602 | MLN9708 | *** | |
A10600 | Ixazomib (MLN2238) | **** | |
A12653 | ONX-0914 (PR-957) | ** | |
A14181 | Oprozomib (ONX 0912) | ** | |
A11145 | Delanzomib (CEP-18770) | *** | |
A10192 | Celastrol | * | |
A13650 | VR23 | **** | |
A14146 | PI-1840 | ** | |
A12730 | Epoxomicin |
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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(R)-MG-132
Catalog No. A21980 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. Learn More -
Ixazomib citrate
Catalog No. A18017 20S proteasome inhibitorIxazomib 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. Learn More -
Proteasome-IN-1
Catalog No. A12254 proteasome inhibitorProteasome-IN-1 is a proteasome inhibitor extracted from patent WO 2013142376 A1. Learn More -
ML604440
Catalog No. A18826 proteasome β1i (LMP2) subunit inhibitorML604440 is a potent, specific and cell permeable proteasome β1i (LMP2) subunit inhibitor. Learn More -
VR23
Catalog No. A13650 Proteasome inhibitorVR23 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 -
Epoxomicin
Catalog No. A12730 Proteasome inhibitorEpoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome. Learn More -
AM 114
Catalog No. A14922 20S proteasome inhibitorAM 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 -
Marizomib (NPI-0052, salinosporamide A)
Catalog No. A13853 Proteasome InhibitorMarizomib is a naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity. Learn More -
MG-262
Catalog No. A12220 Proteasome inhibitorMG-262, a boronic peptide acid, is a potent proteasome inhibitor that selectively and reversibly inhibits the chymotryptic activity of the proteasome. Learn More -
MG-115
Catalog No. A11601 Reversible Proteasome InhibitorMG-115 is a potent, reversible peptide aldehyde inhibitor of proteasome chymotrypsin-like and caspase-like activities. It induces p53 dependent apoptosis. Learn More -
Clasto-Lactacystin b-lactone
Catalog No. A15427 20S proteasome inhibitorClasto-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 -
Dihydroeponemycin
Catalog No. A14932 Proteasome inhibitorDihydroeponemycin is an inhibitor of proteasome and antitumor reagent. Learn More -
Aclacinomycin A
Catalog No. A14910 20S proteasome inhibitorAclarubicin A, an anthracycline drug, specific inhibitor of the 20S proteasome chymotrypsin-like activity. Learn More -
MLN9708
Catalog No. A10602 Proteasome InhibitorMLN9708 is a proteasome inhibitor, which inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome. Learn More -
PI-1840
Catalog No. A14146 reversible proteasome inhibitorPI-1840 is a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity. Learn More -
ONX 0912 (Oprozomib)
Catalog No. A14181 Proteasome inhibitorONX 0912 is a tripeptide epoxyketone, which inhibits growth and induces apoptosis in MM cells resistant to conventional and bortezomib therapies. Learn More -
PSI
Catalog No. A14048 Proteasome inhibitorPSI is a proteasome inhibitor that inhibits chymotrypsin-like activity of the proteasome. Learn More -
Gliotoxin
Catalog No. A13711 20S proteasome inhibitorGliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains of Aspergillus and other fungi. Learn More -
Lactacystin
Catalog No. A12768 proteasome inhibitorLactacystin is a cell-permeable, potent and selective proteasome inhibitor. Learn More -
ONX-0914
Catalog No. A12653 Immunoproteasome inhibitorONX 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 -
PR-171 (Carfilzomib)
Catalog No. A11278 Proteasome inhibitorPR-171 (Carfilzomib) is a tetrapeptide epoxyketone and a selective proteasome inhibitor. It is an analog of epoxomicin. Learn More -
CEP-18770 (Delanzomib)
Catalog No. A11145 Proteasome inhibitorCEP-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 -
MLN2238 (Ixazomib)
Catalog No. A10600 Proteasome InhibitorMLN2238 is a potent reversible and specific β5 site of the 20S proteasome inhibitor with an IC50 value of 3.4 nM. Learn More -
MG-132
Catalog No. A11043 Proteasome inhibitorMG-132 is a potent cell-permeable inhibitor of proteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 μM). Learn More -
Bortezomib (Velcade)
Catalog No. A10160 Proteasome inhibitorBortezomib is a highly selective, reversible inhibitor of the 26S proteasome Learn More