| S2619 |
MG132
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MG132 ((S,R,S)-(-)-MG132, Z-Leu-D-Leu-Leu-al) is a potent proteasome (ChTL, TL, and PGPH) inhibitor. This compound also inhibits calpain (IC50=1.2 μM). It can be used to induce animal models of Parkinson’s disease.
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J Proteomics, 2026, 322:105536
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Nature, 2025, 10.1038/s41586-025-09709-1
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Signal Transduct Target Ther, 2025, 10(1):26
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| S1013 |
Bortezomib
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Bortezomib is a potent 20S proteasome inhibitor with Ki of 0.6 nM. It exhibits favorable selectivity towards tumor cells over normal cells. This compound 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.
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J Proteomics, 2026, 322:105536
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Signal Transduct Target Ther, 2025, 10(1):81
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Cell Host Microbe, 2025, 33(4):512-528.e7
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| S2853 |
PR-171 (Carfilzomib)
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Carfilzomib (PR-171) is an irreversible proteasome inhibitor with IC50 of <5 nM in ANBL-6 cells, displayed preferential in vitro inhibitory potency against the ChT-L activity in the β5 subunit, but little or no effect on the PGPH and T-L activities. Carfilzomib activates prosurvival autophagy and induces cell apoptosis.
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Nat Genet, 2025, 57(10):2468-2481
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Nat Commun, 2025, 16(1):765
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Acta Biomater, 2025, S1742-7061(25)00677-4
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| S2180 |
MLN2238 (Ixazomib)
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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.
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Nat Commun, 2025, 16(1):3138
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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Biomed Pharmacother, 2025, 184:117878
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| S7038 |
Epoxomicin (BU-4061T)
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Epoxomicin (BU-4061T, Aids010837) is a selective proteasome inhibitor with anti-inflammatory activity, which primarily inhibits 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. This compound promotes apoptosis and can be used to induce animal models of Parkinson's Disease.
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Autophagy, 2025, 1-21.
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Am J Hum Genet, 2025, 112(2):374-393
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Acta Neuropathol, 2024, 148(1):14
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| S7049 |
Oprozomib
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Oprozomib is an orally bioavailable inhibitor for CT-L activity of 20S proteasome β5/LMP7 with IC50 of 36 nM/82 nM. Phase 1/2.
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Biosci Rep, 2023, 43(1)BSR20222102
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Microbiol Spectr, 2023, 11(5):e0190423
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Microbiol Spectr, 2023, 10.1128/spectrum.01904-23
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| S1290 |
Celastrol
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Celastrol is a potent proteasome inhibitor for the chymotrypsin-like activity of a purified 20S proteasome with IC50 of 2.5 μM. This compound induces apoptosis and autophagy via the ROS/JNK signaling pathway. It inhibits dopaminergic neuronal death of Parkinson's disease through activating mitophagy.
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World J Gastroenterol, 2025, 31(23):106949
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Adipocyte, 2025, 14(1):2548787
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MedComm (2020), 2024, 5(12):e70033
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| S7172 |
ONX-0914 (PR-957)
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ONX-0914 (PR-957) is a potent and selective immunoproteasome inhibitor, and this compound shows minimal cross-reactivity for the constitutive proteasome in a cell-free assay.
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Nat Commun, 2025, 16(1):765
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Adv Sci (Weinh), 2024, 11(44):e2405318
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J Neurochem, 2024, 10.1111/jnc.16165
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| S1157 |
Delanzomib
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Delanzomib 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.
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Cell Rep Med, 2025, S2666-3791(25)00102-8
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Int J Mol Med, 2025, 55(5)69
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J Fungi (Basel), 2022, 8(2)92
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| S4432 |
Ixazomib Citrate (MLN9708)
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Ixazomib Citrate (MLN9708) 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.
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J Exp Clin Cancer Res, 2022, 41(1):249
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Cell Death Dis, 2022, 13(3):197
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Front Pharmacol, 2022, 13:1032975
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