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DUB

Deubiquitinating enzymes (DUBs), also known as deubiquitinating peptidases, deubiquitinating isopeptidases, deubiquitinases, ubiquitin proteases, ubiquitin hydrolases, ubiquitin isopeptidases, are a large group of proteases that cleave ubiquitin from proteins and other molecules. Ubiquitin is attached to proteins in order to regulate the degradation of proteins via the proteasome and lysosome; coordinate the cellular localisation of proteins; activate and inactivate proteins; and modulate protein-protein interactions.DUBs can reverse these effects by cleaving the peptide or isopeptide bond between ubiquitin and its substrate protein. In humans there are nearly 100 DUB genes, which can be classified into two main classes: cysteine proteases and metalloproteases. The cysteine proteases comprise ubiquitin-specific proteases (USPs), ubiquitin C-terminal hydrolases (UCHs), Machado-Josephin domain proteases (MJDs) and ovarian tumour proteases (OTU). The metalloprotease group contains only the Jab1/Mov34/Mpr1 Pad1 N-terminal+ (MPN+) (JAMM) domain proteases.

  • IMP-1710
    T375912383117-96-0In house
    IMP-1710 is a selective UCH-L1 inhibitor with an IC50 value of 38 nM in a fluorescence polarization assay.
    • $298
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  • USP25/28 inhibitor AZ1
    T76852165322-94-9
    USP25/28 inhibitor AZ1 (AZ1) (AZ1) is an inhibitor of ubiquitin specific protease (USP) 25/28
    • $46
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  • MF-094
    T120242241025-68-1
    MF-094 is a potent and selective inhibitor of USP30 (IC50 of 120 nM).
    • $36
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  • USP8-IN-2
    T678762477651-11-7
    USP8-IN-2 is a potent inhibitor of the deubiquitinating enzymes USP7 and USP8, with an IC50 of 4.0 μM against USP8D. USP8-IN-2 is a potential compound for the treatment of cancer and viral infections.
    • $117
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  • P22074
    T2828490680-28-7In house
    P22074 is a USP7 inhibitor. It is not an active antagonist like its halogenated related compounds. p22074 has antitumour activity.
    • $350
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  • USP28-IN-3
    T747932931509-14-5In house
    USP28-IN-3 is a highly selective USP28 inhibitor with an IC50 value of 0.1 μM against USP28.USP28-IN-3 exhibits anticancer activity and inhibits USP2, USP7, USP8, USP9x, UCHL3, and UCHL5.USP28-IN-3 is cytotoxic to human colorectal and lung squamous carcinoma cells, inhibiting c-cells and c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-neutralizing c-cells through the ubiquitin-proteasome system. -proteasome system to dose-dependently downregulate cellular levels of c-Myc.
    • $293 TargetMol
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  • USP28-IN-4
    T747942931509-15-6
    USP28-IN-4 is a potent USP28 inhibitor with an IC50 value of 0.04 μM against USP28. USP28-IN-4 exhibits anticancer activity and inhibits USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-4 is cytotoxic to human colorectal and lung squamous carcinoma cells and dose-dependently downregulates c-Myc cellular levels through the ubiquitin-proteasome system. -proteasome system to dose-dependently downregulate cellular levels of c-Myc.
    • $293
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  • OTUB1/USP8-IN-1 HCl
    T72784L In house
    OTUB1/USP8-IN-1 HCL is a potent dual inhibitor of OTUB1 and USP8 with potential antitumour activity, inhibiting both OTUB1 and USP8. OTUB1/USP8-IN-1 may be used in the study of leukaemia.
    • $162
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  • OTUB1/USP8-IN-1
    T727842858800-98-1In house
    OTUB1/USP8-IN-1 is a potent OTUB1/USP8 inhibitor with potential anticancer activity, with IC50 values of 0.17 and 0.28 nM for OTUB1 and USP8, respectively.OTUB1/USP8-IN-1 can be used in the study of non-small-cell lung cancer.
    • $100
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  • USP15-IN-1
    T615752260826-16-0In house
    USP15-IN-1 is a potent USP15 inhibitor (IC50 is 3.76 μM). USP15-IN-1 showed high antiproliferative activity against non-small cell lung cancer and leukemia cells. USP15 is an interacting protein of cGAS, and USP15 can promote cGAS to recognize DNA and activate downstream signaling pathways.
    • $128
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  • USP30 inhibitor 18
    T366822242582-40-5In house
    USP30 inhibitor 18 is a selective USP30 inhibitor with an IC50 of 0.02 μM. USP30 inhibitor 18 increases protein ubiquitination and accelerates mitophagy[1]. [1]. Arthur F Kluge, et al. Novel highly selective inhibitors of ubiquitin specific protease 30 (USP30) accelerate mitophagy. Bioorg Med Chem Lett. 2018 Aug 15;28(15):2655-2659.
    • $147
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  • USP30 inhibitor 11
    T132672067332-64-1In house
    USP30 inhibitor 11 (USP30-IN-11) is a selective USP30 inhibitor (IC50: 0.01 µΜ) that inhibits SVA and can be used in studies of cancer, mitochondrial dysfunction and Parkinson's.
    • $215
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  • USP1-IN-2
    T635182098212-05-4In house
    USP1-IN-2 is a potent USP1 inhibitor with potential anti-tumor activity for the study of cancer.
    • $293
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  • SJB3-019A
    T129262070015-29-9In house
    SJB3-019A is a potent, potent and novel ubiquitin-specific protease 1 (USP1) inhibitor, which promotes ID1 degradation and cytotoxicity in K562 cells 5 times more than SJB2-043, with IC50 of 0.0781 μM. SJB3-019A inhibits cell proliferation and causes cell apoptosis.
    • $95
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  • Vialinin A
    T22168858134-23-3In house
    Vialinin A (Terrestrin A), a p-terphenyl compound, exhibits antioxidant properties and acts as a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Its efficacy in autoimmune diseases and cancer research is noteworthy, highlighting its potential therapeutic applications.
    • $213
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  • P005091
    T6925882257-11-6
    P005091 (P5091) is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with EC50 of 4.2 μM.
    • $39
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  • Degrasyn
    T6300856243-80-6
    Degrasyn (WP1130) (WP1130), a specific deubiquitinase (DUB: USP5, UCH-L1, USP9x, USP14, and UCH37) inhibitor, also inhibits Bcr/Abl, which is a JAK2 transducer (without affecting 20S proteasome) and activator of transcription (STAT).
    • $58
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  • ML364
    T35551991986-30-1
    ML364 is an inhibitor of ubiquitin specific peptidase 2 (USP2) and can be used for the research of breast cancer.
    • $66
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  • P 22077
    T24241247819-59-5
    P 22077 (P22077) is an inhibitor of ubiquitin-specific protease USP7 with EC50 of 8.6 μM. It also inhibits the closely related USP47.
    • $32
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  • BAY 11-7082
    T190219542-67-7
    BAY 11-7082 (BAY 11-7821) is an NF-κB inhibitor that inhibits TNFα-induced IκBα phosphorylation (IC50=10 μM). BAY 11-7082 is also an inhibitor of the ubiquitin-specific proteases USP7 and USP21 (IC50=0.19/0.96 μM).
    • $43
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  • Spautin-1
    T19371262888-28-7
    Spautin-1 is a novel autophagy inhibitor, IM inhibited the growth of K562 cells with IC50 of 1.03 μM. In contrast, co-treatment with Spautin-1 increased IM-induced inhibition of cell viability with IC50 of 0.45 μM.
    • $33
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  • LDN-91946
    T15729439946-22-2
    LDN-91946 is an effective and selective inhibitor of ubiquitin C-terminal hydrolase-L1 (UCH-L1) (Ki = 2.8 μM).
    • $39
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  • USP7-IN-1
    T132681381291-36-6
    USP7-IN-1 is a selective and reversible ubiquitin-specific protease 7 (USP7) inhibitor (IC50 = 77 μM).
    • $163
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  • Wu-5
    T777632630378-05-9
    Wu-5 is a potent USP10 inhibitor that inhibits FLT3 and AMPK pathways, promoting the breakdown of FLT3-ITD and inducing apoptosis.
    • $76
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  • RA-9
    T8464919091-63-7
    RA-9 is a potent and selective proteasome-associated inhibitor of deubiquitinating enzymes (DUBs), with favorable toxicity profile and anticancer activity. RA-9 selectively induces apoptosis in ovarian cancer cell lines.
    • $38
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  • DUB-IN-3
    T11112924296-17-3
    DUB-IN-3 is a potent deubiquitinase (USP) enzyme inhibitor and the IC50 for USP8 is 0.56 μM.
    • $139
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  • USP8-IN-3
    T678732477651-10-6
    USP8-IN-3 is a potent inhibitor of the deubiquitinating enzymes USP7 and USP8, with IC50 of 4.0 μM against USP8D. USP8-IN-3 inhibited the proliferation of GH3 and H1957 cells with GI50 values of 37.03 μM and 6.01 μM, respectively. USP8-IN-3 is a potential compound for the treatment of cancer and viral infections.
    • $30
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  • SJB2-043
    T767863388-44-3
    SJB2-043 is an inhibitor of USP1-UAF1 ( IC50 : 544 nM).
    • $47
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  • GNE-6640
    T54612009273-67-8
    GNE-6640 is a non-covalent inhibitor targeting ubiquitin specific peptidase 7 (USP7), exhibiting IC50 values of 0.75 μM for full-length USP7, 0.43 μM for the USP7 catalytic domain, 20.3 μM for full-length USP43, and 0.23 μM for Ub-MDM2, respectively.
    • $64
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  • I-138
    T735602098211-50-6
    I-138 is an orally active and potent reversible inhibitor of USP1-UAF1.I-138 induces mono-ubiquitination of FANCD2 and PCNA and inhibits USP1 auto-cleavage in cells.
    • $198
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  • USP7-IN-8
    T92172009273-60-1
    Benzamide, 4-[6-amino-4-ethyl-5-(4-hydroxyphenyl)-3-pyridinyl]-N-methyl- is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 1.4 μM. USP7-IN-8 (GNE-6776) has anticancer effects.
    • $67
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  • PR-619
    T18622645-32-1
    PR-619 (2,6-Diamino-3,5-dithiocyanopyridine) is a non-selective, reversible inhibitor of the deubiquitinylating enzymes (DUBs).
    • $45
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  • LDN-57444
    T1924668467-91-2
    LDN-57444 is a reversible, competitive proteasome Uch-L1 inhibitor(IC50=0.88 μM) .
    • $34
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  • FT827
    T153511959537-86-0
    FT827 is a covalent inhibitor of selective ubiquitin-specific protease 7 (USP7) (Ki=4.2 µM, Kd=7.8 µM) targeting the catalytic center of the autoinhibitory apolipoprotein form of USP7 for cancer research.
    • $397
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  • USP7-IN-5
    T132702166599-74-0
    USP7-IN-5 is a potent inhibitor of ubiquitin-specific protease 7 (USP7, IC50: 49.9 nM).
    • $2,570
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  • USP7/USP47 inhibitor
    T43381247825-37-1
    USP7/USP47 inhibitor (USP7/47 inhibitor-1) is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively.
    • $40
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  • TCID
    T669730675-13-9
    TCID (UCH-L3 Inhibitor)(IC50=0.6 μM) is a DUB inhibitor of ubiquitin C-terminal hydrolase L3. It has the 125-fold selectivity to L1.
    • $33
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  • HBX 41108
    T21527924296-39-9
    HBX 41108 (HBX-41108) is a non-competitive, reversible inhibitor of USP7 with an IC50 of 424nM. HBX 41108 inhibited deubiquitination of p53 mediated by USP7 in a dose-dependent manner with an IC50 of 0.8μM.
    • $47
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  • B-AP15
    T19321009817-63-3
    B-AP15 (NSC-687852)(NSC-687852) is a selective inhibitor of the deubiquitinating enzymes Usp14 and UCHL5 of the 26S proteasome. It blocks the deubiquitinating activity of the 26S proteasome.
    • $32
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  • KSQ-4279
    T600392446480-97-1
    KSQ-4279 (USP1-IN-1) is an inhibitor of USP1 and PARP.KSQ-4279 has anticancer activity and is used in the study of non-small cell lung cancer, osteosarcoma, ovarian, breast, glioblastoma, bladder, uterine and pancreatic cancers.
    • $158
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  • N-Ethylmaleimide
    T3088128-53-0
    N-Ethylmaleimide (NEM) is a sulfhydryl reagent that is widely used in experimental biochemical studies.
    • $39
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  • USP8-IN-1
    T601462477650-96-5
    USP8-IN-1 is an inhibitor of USP8 with an IC 50 of 1.9 μM. USP8-IN-1 inhibits H1975 cell growth with a GI 50 of 82.04 μM [1].
    • $87
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  • DUB-IN-1
    T11110924296-18-4
    DUB-IN-1, with an IC50 value of 0.24 for USP8, is an active inhibitor of ubiquitin-specific protease (USPs).
    • $98
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  • USP7-IN-6
    T132712166586-47-4
    USP7-IN-6 is a potent inhibitor of ubiquitin-specific protease 7 (USP7, IC50: 6.8 nM).
    • $2,720
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  • GNE-6776
    T46342009273-71-4
    GNE-6776 is a selective USP7 inhibitor.
    • $74
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  • XL177A
    T91222417089-74-6
    XL177A is a selective irreversible USP7 inhibitor(IC50 : 0.34 nM). XL177A elicits cancer cell killing through a p53-dependent mechanism.
    • $97
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  • GSK2643943A
    T114852449301-27-1
    GSK2643943A is a deubiquitylating enzyme (DUB) inhibitor, with an IC 50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy.
    • $38
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  • ML-323
    T17571572414-83-5
    ML323 is a reversible and effective USP1-UAF1 inhibitor in a Ub-Rho assay (IC50: 76 nM) and in orthogonal gel-based assays using K63-linked diubiquitin (di-Ub) (IC50: 174 nM 820 nM)and monoubiquitinated PCNA (Ub-PCNA) (IC50: 820 nM) as substrates, respectively.
    • $52
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  • STD1T
    T36970893075-58-6
    STD1T is a selective and potent inhibitor of the deubiquitinase USP2a with potential anticancer activity that reduces cell cycle protein D1 protein levels in HCT116 colon and MCF-7 breast cancer cells.
    • $225
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  • USP7-IN-3
    T132692202738-42-7
    USP7-IN-3 is a potent and selective allosteric inhibitor of ubiquitin-specific protease 7 (USP7).
    • $2,120
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