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Proteasome
T1176 Racecadotril Racecadotril has been investigated for the basic science and treatment of Diarrhea, Acute Diarrhea, and Acute Gastroenteritis.
T1795 Carfilzomib (PR-171) Carfilzomib is an irreversible proteasome inhibitor and antineoplastic agent that is used in treatment of refractory multiple myeloma.
T2016 MLN9708 MLN2238 suppresses the chymotrypsin-like proteolytic (β5) site of the 20S proteasome(Ki50=0.93 nM, IC50=3.4 nM/). The biologically active form of MLN9708 is MLN2238 in aqueous solutions or plasma.
T2122 MLN2238(Ixazomib) MLN2238, a second generation, boron-containing peptide proteasome inhibitor (PI), inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome (IC50/Ki: 3.4/0.93 nM, in cell-free assays), also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites (IC50: 31/3500 nM).
T2154 MG-132 MG-132 is an inhibitor of proteasome.
T2370 AC-55541 AOB2796 is a novel PAR2 agonist; activated PAR2 signaling in cellular proliferation assays, phosphatidylinositol hydrolysis assays, and Ca(2+) mobilization assays, with potencies ranging from 200 to 1000 nM.
T2399 Bortezomib Bortezomib (PS-341) is a potent 20S proteasome inhibitor (Ki: 0.6 nM, in a cell-free assay). By blocking the targeted proteolysis normally performed by the proteasome, bortezomib disrupts various cell signaling pathways, leading to cell cycle arrest, apoptosis, and inhibition of angiogenesis.
T2583 Cilastatin Cilastatin is a renal dehydropeptidase-I and leukotriene D4 dipeptidase inhibitor. Since the antibiotic, IMIPENEM, is hydrolyzed by dehydropeptidase-I, which resides in the brush border of the renal tubule, cilastatin is administered with imipenem to increase its effectiveness. The drug also inhibit
T3028 Celastrol Celastrol is an effective proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome(IC50=2.5 μM) with antioxidant and anti-inflammatory activity.
T3359 Aprotinin Aprotinin a broad-spectrum serine protease inhibitor, inhibiting the activity of a number of different esterases and proteases, including trypsin, chymotrypsin, kallikrein, plasmin, tissue plasminogen activator, and tissue and leukocytic proteinases.
T4467 UAMC 00039 dihydrochloride UAMC00039 dihydrochloride is a potent, reversible and competitive dipeptidyl peptidase II inhibitor with an IC50 of 0.48 nM.
T6027 CEP-18770 (Delanzomib) CEP-18770 is an orally active inhibitor of the chymotrypsin-like activity of proteasome (IC50: 3.8 nM). It only marginally inhibits the tryptic and peptidylglutamyl activities of the proteosome.
T6029 ONX-0914 ONX-0914 is an effective and specific immunoproteasome inhibitor, which has minimal cross-reactivity for the constitutive proteasome.
T6041 Oprozomib (ONX 0912) Oprozomib (ONX 0912) ,an inhibitor for CT-L activity of 20S proteasome β5(IC50=36 nM)/LMP7(IC50=82 nM), is orally bioavailable. Oprozomib also has potential antineoplastic activity.
T6830 Epoxomicin Epoxomicin is a selective proteasome inhibitor with anti-inflammatory activity, inhibits primarily the CH-L activity of the 20S proteasome, while T-L and PGPH catalytic activities are also inhibited at 100- and 1000-fold reduced rate.
T6941 PI-1840 PI-1840( IC50 = 27 nM)is a reversible and selective chymotrypsin-like (CT-L) inhibitor,with little proteasome proteolytic effects on trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L).
T6999 Teneligliptin hydrobromide Teneligliptin is a novel, potent, and long-lasting dipeptidyl peptidase-4 inhibitor; competitively inhibited human plasma, rat plasma, and human recombinant DPP-4 in vitro, with IC50 values of approximately 1 nM.
T7016 VR23 VR23 is a potent proteasome inhibitor. Data shows IC50 =1 nM for trypsin-like proteasomes, IC50=50-100 nM for chymotrypsin-like proteasomes, and IC50=3 μM for caspase-like proteasomes.
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