20S proteasome 选择性抑制剂

目录号 产品名 产品描述 Selective / Pan IC50 / Ki
S1013 Bortezomib (PS-341) Bortezomib (PS-341, Velcade, LDP-341, MLM341, NSC 681239) is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. Bortezomib (PS-341) inhibits NF-κB and induces ERK phosphorylation to suppress cathepsin B and inhibit the catalytic process of autophagy in ovarian cancer and other solid tumors. Selective 20S proteasome, Ki: 0.6 nM
S4432 Ixazomib Citrate (MLN9708) Ixazomib citrate (MLN9708, Ninlaro) is a prodrug of Ixazomib (MLN2238), which is a selective, orally bioavailable inhibitor of 20S proteasome that inhibits the chymotrypsin-like proteolytic (β5) site with IC50 of 3.4 nM and Ki of 0.93 nM, respectively. Ixazomib (MLN2238) also inhibits caspase-like (β1) and trypsin-like (β2) proteolytic sites with IC50 of 31 nM and 3500 nM, respectively. Selective 20S proteasome β2 site, IC50: 3500 nM; 20S proteasome β5 site, Ki: 0.93 nM; 20S proteasome β1 site, IC50: 31 nM; 20S proteasome β5 site, IC50: 3.4 nM
S2180 Ixazomib (MLN2238) Ixazomib (MLN2238) inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM in cell-free assays, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM. Ixazomib (MLN2238) induces autophagy. Phase 3. Selective 20S proteasome, Ki: 0.93 nM; 20S proteasome, IC50: 3.4 nM
S2181 Ixazomib Citrate (MLN9708) Analogue Ixazomib Citrate (MLN9708) Analogue is the analogue of Ixazomib Citrate (MLN9708) from WO2016165677A1. Ixazomib Citrate (MLN9708) immediately hydrolyzed to Ixazomib (MLN2238), the biologically active form, on exposure to aqueous solutions or plasma. Ixazomib (MLN2238) inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50/Ki of 3.4 nM/0.93 nM in cell-free assays, less potent to β1 and little activity to β2. Ixazomib (MLN2238) induces auto Selective 20S proteasome, IC50: 3.4 nM; 20S proteasome, Ki: 0.93 nM
S7504 Salinosporamide A (NPI-0052) Salinosporamide A (NPI-0052, ML858, Marizomib, MRZ) is a novel marine derived proteasome inhibitor which inhibits CT-L β5, C-L β1, and T-L β2 proteasome activities in human erythrocyte-derived 20S proteasomes with IC50 of 3.5 nM, 430 nM, 28 nM. Selective C-L β1, IC50: 430 nM; T-L β2, IC50: 28 nM; CT-L β5, IC50: 3.5 nM
S1157 Delanzomib (CEP-18770) Delanzomib (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. Phase 1/2. Selective Chymotrypsin-like proteasome, IC50: 3.8 nM
S7172 ONX-0914 (PR-957) ONX-0914 (PR-957) is a potent and selective immunoproteasome inhibitor with minimal cross-reactivity for the constitutive proteasome in a cell-free assay. Selective LMP7, IC50: ~10 nM
S7462 PI-1840 PI-1840 is a reversible and selective chymotrypsin-like (CT-L) inhibitor with IC50 of 27 nM with little effects on the other two major proteasome proteolytic activities, trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L). Selective Chymotrypsin-like proteasome, IC50: 27 nM
S7049 Oprozomib (ONX 0912) Oprozomib (ONX 0912, PR-047) is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2. Selective 20S proteasome LMP7, IC50: 82 nM; 20S proteasome β5, IC50: 36 nM
S1290 Celastrol (NSC 70931) Celastrol (NSC 70931, Tripterine) is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy. Selective 20S proteasome, IC50: 2.5 μM
S7038 Epoxomicin (BU-4061T) Epoxomicin (BU-4061T, Aids010837) 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. Epoxomicin promotes apoptosis. Selective