Deubiquitinase
DUBs
Deubiquitinases (DUBs) are a family of proteases whose function is to cleave ubiquitin (Ub) or ubiquitin-like proteins from proproteins or ubiquitin(s) conjugated with target substrate. DUBs are divided into two main classes according to their enzymatic cleavage mechanism: cysteine proteases and zinc metalloproteases. These include ubiquitin-specific proteases (USPs), ubiquitin C-terminal hydrolases (UCHs), ovarian tumor proteases (OTUs), Machado-Joseph disease proteases (MJDs), Jab1/Mov34/Mpr1 (JAMM) metalloproteases, and MIU-containing novel DUB family, (MINDY) proteases.
Ubiquitination is an important post-translational modification that plays a key role in many vital cellular events. In this process, ubiquitin is attached to a substrate protein by the concerted action of an enzyme cascade involving E1, E2 and E3 enzymes and it is removed by DUBs. DUBs are therefore important regulators of the Ub system and regulate a plethora of cellular processes, including protein turnover, protein sorting, and trafficking. Altered DUB activity is associated with a multitude of pathologies including cancer. DUBs represent novel candidates for target-directed drug development.
Deubiquitinase Isoform Specific Products
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Deubiquitinase
(142)
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USP1
(13)
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USP2
(3)
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USP4
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USP7
(23)
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USP8
(4)
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USP10
(4)
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USP21
(3)
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USP30
(6)
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UCHL1
(4)
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USP11
(1)
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USP15
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USP28
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USP25
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All Product Categories
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Deubiquitinase Inhibitors
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Deubiquitinase Agonist
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Deubiquitinase Antagonist
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Deubiquitinase Activator
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Deubiquitinase Chemical
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Deubiquitinase Degraders
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Deubiquitinase Ligands
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Deubiquitinase Proteins
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Deubiquitinase Related Products (212)
Related Products (212)
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Recombinant Proteins (48)
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Antibodies (16)
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Deubiquitinase Isoform Comparison
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DUB-IN-3
0 ImagesDUB-IN-3 (compound 22c) is a potent and selective inhibitor of the deubiquitinating enzyme USP8 with an IC50 value of 0.56 μM. DUB-IN-3 is promising for research of cancer, neurodegenerative diseases, inflammation, viral infection and cardiovascular disease.
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BC-1471
0 ImagesBC-1471 is a STAMBP deubiquitinase inhibitor with an IC50 of 0.33 μM. BC-1471 can inhibit the activity of the NALP7 inflammasome. BC-1471 has anti-inflammatory activity and can be used for the research of inflammatory diseases.
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OTUB1/USP8-IN-1 TFA
0 ImagesCat. No.: HY-151563APurity: 99.56%OTUB1/USP8-IN-1 TFA is the TFA salt form of OTUB1/USP8-IN-1 (HY-151563). OTUB1/USP8-IN-1 TFA is a dual inhibitor for OTUB1/USP8, IC50 for OTUB1 and USP8 is 0.17 and 0.28 nM, respectively. OTUB1/USP8-IN-1 TFA inhibits proliferation of NSCLC cells. OTUB1/USP8-IN-1 TFA exhibits good pharmacokinetic characters in ICR mouse, and exhibits antitumor activity in H1975 xenograft mouse model.
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IU1-248
0 ImagesIU1-248, a derivative of IU1, is a potent and selective USP14 inhibitor with an IC50 of 0.83 μM.
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U7D-1
0 ImagesU7D-1 is a USP7 PROTAC degrader that induces selective proteasomal degradation of USP7. U7D-1 destabilizes and downregulates the expression of variant PRC1 complex subunits PCGF1, RING1A and PCGF6, and also slightly reduces the protein level of KDM2B. U7D-1 decreases cell viability, arrests neuroblastoma cells at the G0/G1 cell cycle phase, and downregulates the expression of target genes of PAX3::FOXO1 in FP-RMS cells. U7D-1 increases the level of cleaved PARP in FP-RMS cells, induces cell apoptosis, and upregulates the expression of muscle differentiation markers MYH1 and MYF5. U7D-1 inhibits the growth and proliferation of p53 wild-type and mutant cancer cells, and regulates the apoptosis pathway and E2F pathway. U7D-1 is applicable to studies on neuroblastoma, fusion-positive rhabdomyosarcoma, p53-mutant cancers and cancer-related research.
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Subquinocin
0 ImagesCat. No.: HY-176426Purity: 98.27%Subquinocin is a tumor suppressor CYLD inhibitor that inhibits USP family deubiquitinases (DUBs) activity of CYLD with an IC50 of 30 μM. Subquinocin enhances the activation of NF-κB and IFN pathways by inhibiting CYLD. Subquinocin promotes RIG-I-mediated activation of IRF3/IRF7 in the interferon pathway. Subquinocin can be used for the research of cancer and neurodegenerative diseases.
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PROTAC USP39 Degrader-1
0 ImagesCat. No.: HY-180907Purity: 98.00%PROTAC USP39 Degrader-1 is a USP39 PROTAC degrader with Kd values of 136 nM and 232 nM, and a DC50 value of 1.06 nM (24 h). PROTAC USP39 Degrader-1 binds to the VHL E3 ubiquitin ligase, forms a ternary complex with USP39, mediates USP39 ubiquitination and proteasomal degradation dependent on VHL recruitment, modulates splicing activity and induces 5' splice site-specific splicing patterns. PROTAC USP39 Degrader-1 can be used in the research of cervical cancer.
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WCY-8-67 TFA
0 ImagesCat. No.: HY-178500APurity: 99.40%WCY-8-67 TFA is an orally active and selective USP5 inhibitor, with an IC50 value of 1.33 μM. WCY-8-67 TFA induces apoptosis and suppresses JAK/STAT3 and PI3K/AKT signaling pathways. WCY-8-67 TFA inhibits proliferation of AE-positive AML cells, induces G1 phase arrest and differentiation of AML cells. WCY-8-67 TFA demonstrates potent anti-leukemic efficacy in mice. WCY-8-67 TFA can be used for the study of acute myeloid leukemia.
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USP7-IN-3
0 ImagesUSP7-IN-3 (Compound 5) is an effective and selective allosteric inhibitor of ubiquitin-specific protease 7 (USP7). USP7-IN-3 can be used for research on acute lymphoblastic leukemia.
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USP7-IN-9
0 ImagesUSP7-IN-9 is a highly potent ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 value of 40.8 nM. USP7-IN-9 can induce apoptosis and arrest cell progression at G0/G1 and S phases in RS4; 11 cells. USP7-IN-9 reduces the protein levels of oncoproteins MDM2 and DNMT1 and increases the protein levels of tumor suppressors p53 and p21.
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6-Thioguanine (Standard)
0 ImagesSynonyms: Thioguanine (Standard); 2-Amino-6-purinethiol (Standard)6-Thioguanine (Standard) is the analytical standard of 6-Thioguanine. This product is intended for research and analytical applications. 6-Thioguanine (Thioguanine; 2-Amino-6-purinethiol) is an anti-leukemia and immunosuppressant agent, acts as an inhibitor of SARS and MERS coronavirus papain-like proteases (PLpros) and also potently inhibits USP2 activity, with IC50s of 25 μM and 40 μM for Plpros and recombinant human USP2, respectively.
