| S3692 |
N-Ethylmaleimide (NEM)
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NEM (N-Ethylmaleimide) is an organic compound that is derived from maleic acid. It is an irreversible inhibitor of all cysteine peptidases, with alkylation occurring at the active site thiol group. N-Ethylmaleimide (NEM) inactivates endogenous deubiquitinating enzymes (DUBs). N-Ethylmaleimide (NEM) specifically inhibits phosphate transport in mitochondria.
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Nat Commun, 2025, 16(1):7812
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Inflammation, 2025, 10.1007/s10753-025-02273-w
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Toxicol Lett, 2025, 406:31-37
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| E2899 |
MG132 SSS
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MG132 SSS(Z-Leu-Leu-Leu-al, MG132) is a potent proteasome and calpain inhibitor with IC50 of 100 nM and 1.2 μM, respectively.
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J Adv Res, 2025, S2090-1232(25)00940-3
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| S7396 |
Calpeptin
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Calpeptin is a potent, cell-permeable calpain inhibitor with ID50 of 52 nM, 34 nM, 138 nM, and 40 nM for Calpain I (porcine erythrocytes), Calpain II (porcine kidney), Papainb, and Calpain I (human platelets), respectively. This compound attenuates apoptosis and intracellular inflammatory changes in muscle cells.
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EMBO Mol Med, 2025, 17(12):3355-3376
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Transl Psychiatry, 2025, 15(1):52
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Mol Med, 2025, 31(1):166
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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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| S7393 |
Aloxistatin (E-64d)
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Aloxistatin (E64d) is an irreversible and membrane-permeable cysteine protease inhibitor with blood platelet aggregation inhibiting activity. The cysteine protease cathepsin L is required for SARS-CoV-2 viral entry, and aloxistatin treatment reduced cellular entry of SARS-CoV-2 pseudovirions by 92.3%.
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Nat Chem Biol, 2025, 10.1038/s41589-025-01907-2
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J Exp Clin Cancer Res, 2025, 44(1):317
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Cell Rep, 2025, 44(4):115507
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| S1115 |
Odanacatib
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Odanacatib is a potent, selective, and neutral inhibitor of cathepsin K (human/rabbit) with IC50 of 0.2 nM/1 nM, and demonstrated high selectivity versus off-target cathepsin B, L, S. Phase 3.
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PLoS One, 2025, 20(7):e0327246
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Int Dent J, 2025, 75(4):100810
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Br J Pharmacol, 2024, 10.1111/bph.17312
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| S7379 |
E-64
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E-64 is an irreversible and selective cysteine protease inhibitor, and also inhibits papain, calpain, and cathepsins B and H, but not serine proteases or aspartic proteases. The IC50 for papain is 9 nM. This compound induces oxidative stress and apoptosis in Filarial Parasite.
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Nat Commun, 2025, 16(1):5403
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Elife, 2025, 14RP104057
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bioRxiv, 2024, 2024.09.30.615241
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| S7386 |
MG-101 (ALLN)
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MG-101 (ALLN, Calpain inhibitor-1, Ac-LLnL-CHO) is a cell-permeable and potent inhibitor of cysteine proteases including calpains and lysosomal cathepsins.
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Cell Biosci, 2024, 14(1):115
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Exp Hematol Oncol, 2023, 12(1):77
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Comput Struct Biotechnol J, 2022, 20:2442-2454
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| S7391 |
Z-FA-FMK
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Z-FA-FMK ((1S)-Z-FA-FMK) is an irreversible cysteine protease inhibitor, and also inhibits effector caspases.
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Eur J Med Chem, 2025, 300:118108
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Cancer Res, 2022, can.21.4222
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Comput Struct Biotechnol J, 2022, 20:2442-2454
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| S2847 |
Cathepsin Inhibitor 1
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Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively.
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bioRxiv, 2025, 2025.09.08.674976
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Cell Mol Life Sci, 2024, 81(1):442
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Elife, 2023, 12e79144
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