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Proteasome

Inhibitory Selectivity
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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Catalog No. Product Name Application Product Information
A14922

AM 114

20S proteasome 抑制剂
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.
A12730

Epoxomicin

Proteasome 抑制剂
Epoxomicin is a potent anti-tumor agent isolated from Actinomycetes that is used as a selective and irreversible inhibitor of the 20S proteasome.
A13650

VR23

Proteasome 抑制剂?€?
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).
A14181 SALE

ONX 0912 (Oprozomib)

proteasome inhibitor
ONX 0912 is a tripeptide epoxyketone, which inhibits growth and induces apoptosis in MM cells resistant to conventional and bortezomib therapies.
A14146

PI-1840

reversible proteasome 抑制剂
PI-1840 is a novel noncovalent and rapidly reversible proteasome inhibitor with anti-tumor activity.
A13853

Marizomib (NPI-0052, salinosporamide A)

Proteasome 抑制剂
Marizomib is a naturally-occurring salinosporamide, isolated from the marine actinomycete Salinospora tropica, with potential antineoplastic activity.
A14910

Aclacinomycin A

20S proteasome 抑制剂
Aclarubicin A, an anthracycline drug, specific inhibitor of the 20S proteasome chymotrypsin-like activity.
A14932

Dihydroeponemycin

Proteasome 抑制剂
Dihydroeponemycin is an inhibitor of proteasome and antitumor reagent.
A15427

Clasto-Lactacystin b-lactone

20S proteasome 抑制剂
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.
A11601

MG-115

Reversible Proteasome 抑制剂
MG-115 is a potent, reversible peptide aldehyde inhibitor of proteasome chymotrypsin-like and caspase-like activities. It induces p53 dependent apoptosis.
A14048

PSI

Proteasome 抑制剂
PSI is a proteasome inhibitor that inhibits chymotrypsin-like activity of the proteasome.
A13711

Gliotoxin

20S proteasome 抑制剂
Gliotoxin is an immunosuppressive mycotoxin produced by pathogenic strains of Aspergillus and other fungi.
A12768

Lactacystin

proteasome 抑制剂
Lactacystin is a cell-permeable, potent and selective proteasome inhibitor.
A12653 SALE

ONX-0914

Immunoproteasome 抑制剂
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.
A11278 SALE

PR-171 (Carfilzomib)

Proteasome 抑制剂
PR-171 (Carfilzomib) is a tetrapeptide epoxyketone and a selective proteasome inhibitor. It is an analog of epoxomicin.
A11145 SALE

CEP-18770

Proteasome 抑制剂
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.
A10600 SALE

MLN2238

Proteasome 抑制剂
MLN2238 is a potent reversible and specific β5 site of the 20S proteasome inhibitor with an IC50 value of 3.4 nM.
A11043 SALE

MG-132

Proteasome 抑制剂
MG-132 is a potent cell-permeable inhibitor of proteasome (IC50 = 100 nM) and calpain (IC50 = 1.2 μM).
A10160 SALE

Bortezomib (Velcade)

Proteasome 抑制剂
Bortezomib is a highly selective, reversible inhibitor of the 26S proteasome
A10602 SALE

MLN9708

Proteasome 抑制剂
MLN9708 is a proteasome inhibitor, which inhibits the activity of the proteasome, blocking the targeted proteolysis normally performed by the proteasome.
A12220

MG-262

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

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