| S6877 |
EOAI3402143
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EOAI3402143 is a dose-dependent inhibitor of Usp9x, Usp24 and Usp5 that increases tumor cell apoptosis, and fully blocks or regresses myeloma tumors in mice.
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Cell Rep Med, 2023, 4(4):101007
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Int J Biol Sci, 2021, 17(10):2417-2429
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Int J Biol Sci, 2021, 17(10):2417-2429
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| S8904 |
USP25/28 inhibitor AZ1
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AZ1 is a potent and noncompetitive dual Inhibitors of the ubiquitin-specific protease (USP) 25/28 with IC50s of 0.62 μM and 0.7 μM in Ub-RH110 assay,respectively.
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Cell Death Dis, 2025, 16(1):305
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Mol Oncol, 2022, 10.1002/1878-0261.13217
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Cancer Sci, 2022, 113-10:3463-3475
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| S6748 |
ML364
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ML364 is a small molecule inhibitor of the deubiquitinase USP2 with an IC50 of 1.1 μM in a biochemical assay using an internally quenched fluorescent di-ubiquitin substrate.
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Nat Commun, 2025, 16(1):4564
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Cell Insight, 2022, 1(4):100047
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J Virol, 2020, JVI.01857-20
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| S0515 |
PLpro inhibitor
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PLpro inhibitor (compound 6) is a potent papain-like protease (PLpro)/deubiquitinase (DUBs) inhibitor with IC50 of 2.6 μM and EC50 of 13.1 μM that blocks SARS virus replication.
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PLoS Pathog, 2023, 19(8):e1011592
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bioRxiv, 2022, 2022.08.06.503039
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| E1479 |
I-138
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I-138 is an orally active, potent reversible inhibitor of USP1-UAF1 with IC50 0f 4.1 nM. This compound is structurally related to ML323 and induces the monoubiquitination of FANCD2 and PCNA in MDA-MB-436 cells and increases PCNA and FANCD2 monoubiquitination in HAP-1 USP1 WT cells.
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J Biol Chem, 2025, 301(3):108190
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| S8967 |
XL177A
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XL177A is a potent, selective and irreversible inhibitor of Ubiquitin specific peptidase 7 (USP7) with IC50 of 0.34 nM.
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Queen's University Belfast, 2023,
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| E1330 |
Usp22i-S02
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Usp22i-S02(USP22-IN-1, compound S02) is a potent inhibitor of ubiquitin specific peptidase 22 (USP22). It showed anticancer activity by suppressing Foxp3 expression in T-regulatory cells.
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Int Immunopharmacol, 2025, 153:114538
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| S6845 |
GRL0617
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GRL0617 is a potent, selective and competitive noncovalent inhibitor of severe acute respiratory syndrome (SARS-CoV) papain-like protease (PLPro)/deubiquitinase with IC50 of 0.6 μM and Ki of 0.49 μM. This compound inhibits SARS-CoV viral replication in Vero E6 cells with EC50 of 15 microM and has no associated cytotoxicity.
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J Virol, 2024, e0085524.
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| S6883 |
HBX 19818
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HBX19818 is a specific inhibitor of USP7 with an IC 50 of 28.1 μM.
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Queen's University Belfast, 2023,
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| S6933 |
GEN-6776
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GNE-6776 is a potent, non-covalent, selective and orally bioavailable inhibitor of USP7 with IC50 of 1.34 μM and 0.61 μM for full length USP7 and USP7 catalytic domain, respectively.
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Queen's University Belfast, 2023,
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| S0399 |
SJB2-043
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SJB2-043 is a potent USP1 inhibitor that inhibits the activity of native USP1/UAF1 with IC50 of 544 nM.
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Front Pharmacol, 2021, 12:695009
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| S6878 |
GSK2643943A
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GSK2643943A is an inhibitor of deubiquitylating enzyme (DUB) with IC50 of 160 nM for USP20/Ub-Rho.
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Nature, 2020, 10.1038/s41586-020-2928-y
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| S4922 |
NSC 632839
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NSC 632839 is not only a DUB inhibitor, but also a deSUMOylase inhibitor, it inhibits USP2, USP7, and SENP2 with EC50 of 45 μM, 37 μM, and 9.8 μM, respectively.
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| E5945New |
Wu-5
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Wu-5 is an inhibitor of USP10 that blocks its activity in vitro with an IC50 of 8.3 µM. It also promotes FLT3-ITD degradation and synergistically enhances crenolanib-induced apoptosis.
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| E1633 |
BAY-805
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BAY-805 is a potent, selective, and cell-active inhibitor that non-covalently targets the catalytic activity of USP21, a member of the ubiquitin-specific protease (USP) subfamily of deubiquitinating enzymes (DUBs).
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| E6502New |
USP7-IN-1
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USP7-IN-1 (Example 2) is a selective and reversible inhibitor of USP7 with an IC50 of 77 Μm and exhibits antiproliferative activity, inhibiting the growth of HCT116 colorectal cancer cells with a GI50 of 67 μM.
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| E5999New |
CT1113
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CT1113 is a potent dual inhibitor of USP25 and USP28 that effectively reduces c-MYC levels and exhibits strong anti-tumor activity. It can be used in research on colon and pancreatic cancers.
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| E1098 |
MF-094
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MF-094, a potent and selective USP30 inhibitor (IC50=0.12 μM), accelerates diabetic wound healing by inhibiting the NLRP3 inflammasome.
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| E0392 |
Dubs-IN-1
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Dubs-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC50 of 0.85 μM for USP8.
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| E0389 |
DUBs-IN-2
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DUBs-IN-2 is a potent inhibitor of USP7 and USP8 deubiquitinating enzymes.
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| E0947 |
Iu1-248
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Iu1-248, a derivative of IU1, is a potent and selective ubiquitin specific peptidase 14 (USP14) inhibitor with an IC50 of 0.83 μM.
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| E1118New |
SJB3-019A
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SJB3-019A is a potent inhibitor of USP1 that significantly suppresses cell proliferation and induces apoptosis in B-cell acute lymphoblastic leukemia (B-ALL) cells. It also promotes DNA-binding-1 (ID1) degradation in K562 cells.
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| S6943 |
IU1-47
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IU1-47 is a potent and specific inhibitor of USP14 with an IC50 of 0.6 μM. This compound shows ∼33-fold selectivity for USP14 over USP5 (IsoT).
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| E6671New |
CMPD-39
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CMPD-39 (Compound 39) is a selective non-covalent inhibitor of USP30 with an IC50 of ~20 nM in in vitro enzyme assays.
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| S0884 |
RA-9
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RA-9 is a cell-permeable, potent and selective inhibitor of proteasome-associated deubiquitinating enzymes (DUBs) with favorable toxicity profile and anticancer activity. This compound selectively induces apoptosis in ovarian cancer cell lines.
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| S2913 |
BAY 11-7082 (BAY 11-7821)
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BAY 11-7082 (BAY 11-7821) is a NF-κB inhibitor, inhibits TNFα-induced IκBα phosphorylation with IC50 of 10 μM in tumor cells. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 with IC50 of 0.19 μM and 0.96 μM, respectively. BAY 11-7082 induces apoptosis and S phase arrest in gastric cancer cells.
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ACS Nano, 2025, 19(20):19057-19079
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Adv Sci (Weinh), 2025, 12(28):e2502634
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J Med Virol, 2025, 97(8):e70534
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| S2243 |
Degrasyn (WP1130)
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Degrasyn (WP1130) is a selective deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor and also suppresses Bcr/Abl, also a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT). This compound induces apoptosis and blocks autophagy.
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Nat Commun, 2025, 16(1):628
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Nat Commun, 2025, 16(1):1313
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Cell Death Dis, 2025, 16(1):564
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| S7888 |
Spautin-1
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Spautin-1 is a potent and specific autophagy inhibitor, and inhibits the deubiquitinating activity of USP10 and USP13 with IC50 of ∼0.6-0.7 μM. This compound enhances apoptosis.
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Nat Commun, 2024, 15(1):9463
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J Adv Res, 2024, S2090-1232(24)00025-0
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Cancer Lett, 2024, 604:217258
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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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