| S7933 |
VR23
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VR23 is a potent proteasome inhibitor with IC50 of 1 nM, 50-100 nM, and 3 μM for trypsin-like proteasomes, chymotrypsin-like proteasomes, and caspase-like proteasomes, respectively.
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Journal of Proteomics, March 30, 2023, 104839
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Molecular Brain, January 8, 2026, 19(1)
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Molecular Brain, 2026, Article in Press
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| S7504 |
Marizomib (Salinosporamide A)
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Marizomib (Salinosporamide A) 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.
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Mol Oncol, 2023, 17(9):1821-1843
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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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| S7462 |
PI-1840
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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).
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Cell Death Discovery, 2024, 57
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Nat Cell Biol, 2022, 24(3):364-372
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Cancer Sci, 2020, 112(1):133-143
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| E7414 |
MG-115
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MG-115 is a potent and reversible inhibitor of proteasomes with ki of 21 nM and 35 nM for the 20S and 26S proteasomes, respectively. It also induces apoptosis in Rat-1 and PC12 cells by selectively inhibiting the chymotrypsin-like activity of the proteasome.
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Neoplasia, 2021, 1213-1226
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Cell Research, 2020, 678-692
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| E1214 |
KSQ-4279 (USP1-IN-1)
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KSQ-4279 (USP1-IN-1) is an orally bioavailable selective inhibitor of the ubiquitin specific protease 1 (USP1) with anti-proliferative activity. KSQ-4279 also exhibits synergistic activity in combination with PARP inhibitors.
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Cancer Res, 2024, 84(20):3419-3434
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Sci Adv, 2024, 10(46):eadp6567
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| S5813 |
Isoginkgetin
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Isoginkgetin is a naturally derived biflavonoid with anti-tumor activity. This compound directly inhibits the chymotrypsin-like, trypsin-like, and caspase-like activities of the 20S proteasome. It also is a general inhibitor of Pre-mRNA splicing.
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Cell Death Dis, 2024, 15(4):289
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| S6851 |
RA-190
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RA190, a bis-benzylidine piperidon, is a potent, selective and oral effective inhibitor of proteasome ubiquitin receptor RPN13/ADRM1 with anticancer activity. RA190 triggers ER stress response, p53/p21 signaling axis and autophagy in multiple myeloma cells.
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| S8279 |
(Rac)-Shikonin
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(±)-Shikonin, a potent and specific Pyruvate kinase M2 (PKM2) inhibitor, is a major component of zicao (purple gromwell, the dried root of Lithospermum erythrorhizon), a Chinese herbal medicine with various biological activities. It is also an inhibitor of TMEM16A chloride channel activity using cell-based fluorescent-quenching assay. Shikonin exerts an anti-inflammatory effect by inhibiting tumor necrosis factor-α (TNF-α) and prevents activation of nuclear factor-κB (NF-κB) pathway via proteasome inhibition.
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Signal Transduct Target Ther, 2025, 10(1):341
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J Exp Clin Cancer Res, 2025, 44(1):299
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Free Radic Biol Med, 2025, 237:65-75
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| S1290 |
Celastrol (Tripterine)
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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. Celastrol induces apoptosis and autophagy via the ROS/JNK signaling pathway. Celastrol 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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| S3269 |
Acetylcorynoline
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Acetylcorynoline, a major alkaloid component derived from Corydalis bungeana which is a traditional Chinese medical herb, shows anti-inflammatory properties. This compound may decrease egl-1 expression to suppress apoptosis pathways and increase rpn5 expression to enhance the activity of proteasomes.
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