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Proteasome Proteasome

Cat.No.  Name Information
M1902 MG132 MG132 is a specific and potent cell-permeable proteasome inhibitor (IC50 = 100 nM, Ki = 4 nM). MG-132 effectively blocks the proteolytic activity of the 26S proteasome complex. MG-132 is also a calpain inhibitor with IC50 of 1.2 μM.
M2071 ONX-0914 Onx-0914 (PR-957) is a selective inhibitor of low molecular weight polypeptide 7 (LMP7), a chymotrypsin subunit of the immune proteasome. Onx-0914 blocks cytokine production and reduces the progression of experimental arthritis. Onx-0914 is a non-competitive irreversible inhibitor of mycobacterium proteasome (Ki=5.2 μM). Onx-0914 activates latent HIV-1 through HF-1-mediated p-TEFb activation.
M1686 Bortezomib (PS-341) Bortezomib (PS-341) is a highly selective proteasome inhibitor with a ki value of 6nM.
M2193 Epoxomicin Epoxomicin (BU-4061T) is a cell-permeable, selective and irreversible proteasome inhibitor with an IC50 value of 4 nM. Epoxomicin covalently binds to the LMP7, X, MECL1, and Z catalytic subunits of the proteasome and potently inhibits primarily the chymotrypsin-like activity. Epoxomicin can cross the blood-brain barrier.
M2035 IU1 IU1 is a reversible, small molecule inhibitor of deubiquitination by USP14 that demonstrates an IC50 value of 4-5 μM.
M3884 Celastrol Celastrol (Tripterin) is a potent antioxidant and anti-inflammatory agent, as well as a proteasome inhibitor which potently and preferentially inhibits the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM.
M4814 K-7174 dihydrochloride K-7174 dihydrochloride is a novel, orally active proteasome and GATA inhibitor, inhibits the expression of vascular cell adhesion molecule-1 (VCAM-1) induced by either IL-1β or TNF-α.
M3478 Gabexate Mesylate Gabexate Mesylate is a serine protease inhibitor with IC50 of 0.19 μM which is used in the research of pancreatitis and disseminated intravascular coagulation.
M3476 CEP-18770 CEP-18770 is an orally active inhibitor of the chymotrypsin-like activity of proteasome with IC50 of 3.8 nM, with only marginal inhibition of the tryptic and peptidylglutamyl activities of the proteosome.
M2995 Salinosporamide A Salinosporamide A (NPI-0052, Marizomib) is a novel marine derived proteasome inhibitor which inhibits CT-L, C-L, and T-L proteasome activities in human erythrocyte-derived 20S proteasomes with EC50 of 3.5 nM, 430 nM, 28 nM.
M2801 Lactacystin Lactacystin is a potent and selective inhibitor of the 20S proteasome.
M2285 MLN2238 MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM, respectively.
M2152 Carfilzomib Carfilzomib (PR-171) is an irreversible proteasome inhibitor with an IC50 of <5 nM. Carfilzomib irreverently selectively binds to the active site containing n-terminal threonine of the 20S proteasome and proteolytic core particles of the 26S proteasome.*The compound is unstable in solutions, freshly prepared is recommended.
M2150 Oprozomib Oprozomib (ONX 0912) is a novel orally proteasome inhibitor with potential antineoplastic activity.
M2122 MLN9708 MLN9708 is a novel orally bioactive proteasome inhibitor, inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with an IC50 value of 3.4 nM.
M1844 ITMN-191 ITMN-191 (Danoprevir, RG7227) is a potent and orally active inhibitor of hepatitis C virus (HCV) NS3/4A serine protease with an IC50 of 1.6 nM.
M1724 CTP-518 CTP-518 is a novel HIV protease inhibitor. CTP-518 has the potential to be the first HIV protease inhibitor toeliminate the need to co-dose with a boosting agent.
M56779 Proteasome inhibitor IX Proteasome inhibitor IX (PS-IX; AM114) is a Chalcone derivative and a chymotrypsin-like activity of the 20S proteasome inhibitor with an IC50 value of ~1 μM.
M54581 NIC-0102 NIC-0102 is an orally potent proteasome inhibitor (pIC50=7.55) that specifically inhibits NLRP3 inflammasome activation.NIC-0102 showed potent anti-inflammatory effects in vivo in a DSS-induced ulcerative colitis model. In addition, NIC-0102 inhibited the production of pro-IL-1β.
M54168 Ac-WLA-AMC Ac-WLA-AMC is a specific 20S constitutive proteasome β5 fluorogenic substrate.
M53943 Ac-Nle-Pro-Nle-Asp-AMC Ac-Nle-Pro-Nle-Asp-AMC is a specific substrate for 26S proteasome.
M52545 PR-39 PR-39, a natural proline- and arginine-rich antibacterial peptide, is a noncompetitive, reversible and allosteric proteasome inhibitor.
M52544 PSI PSI (Proteasome Inhibitor 1) is a potent proteasome inhibitor.
M52543 Suc-Ala-Ala-Pro-Phe-SBzl Suc-Ala-Ala-Pro-Phe-SBzl can be used as the substrate of rat intestinal mast cell protease (RMCP I), rat skeletal muscle mast cell protease (RMCP II) and Chymotrypsin.
M52542 Ac-Leu-Leu-Norleucinol Ac-Leu-Leu-Norleucinol (ALLN) is a calpain inhibitor, can be used for research of Acetaminophen induced acute liver damage, and lowers glutamic-oxalacetic transaminease (ALT) and glutamic-pyruvic transaminase (AST).
M52541 MeOSuc-Gly-Leu-Phe-AMC MeOSuc-Gly-Leu-Phe-AMC is a peptide substrate of proteasomal.




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