2. Signaling Pathways
  3. Cell Cycle/DNA Damage
  4. Deubiquitinase

Deubiquitinase

DUBs

Deubiquitinase

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-13453
    BAY 11-7082
    		Inhibitor 99.98%
    BAY 11-7082 is an IκBα phosphorylation and NF-κB inhibitor. BAY 11-7082 selectively and irreversibly inhibits the TNF-α-induced phosphorylation of IκB-α, and decreases NF-κB and expression of adhesion molecules. BAY 11-7082 inhibits ubiquitin-specific protease USP7 and USP21 (IC50=0.19, 0.96 μM, respectively). BAY 11-7082 inhibits gasdermin D (GSDMD) pore formation in liposomes and inflammasome-mediated pyroptosis and IL-1β secretion in human and mouse cells.
    BAY 11-7082
  • HY-13814
    PR-619
    		Inhibitor 99.38%
    PR-619 is a broad-range and reversible DUB inhibitor with EC50s of 3.93, 4.9, 6.86, 7.2, and 8.61 μM for USP4, USP8, USP7, USP2, and USP5, respectively. PR-619 induces ER Stress and ER-Stress related apoptosis.
    PR-619
  • HY-12990
    Spautin-1
    		Inhibitor 99.27%
    Spautin-1 is a specific and potent autophagy inhibitor which inhibits ubiquitin-specific peptidases, USP10 and USP13 with IC50s of 0.6-0.7 μM.
    Spautin-1
  • HY-13264
    Degrasyn
    		Inhibitor 99.70%
    Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
    Degrasyn
  • HY-145471
    KSQ-4279
    		Inhibitor 99.94%
    KSQ-4279 (USP1-IN-1) is a potent, first-in-class, and highly selective USP1 inhibitor. KSQ-4279 shows anticancer effects.
    KSQ-4279
  • HY-103435
    Vialinin A
    		Inhibitor ≥99.0%
    Vialinin A (Terrestrin A) is a p-terphenyl compound with antioxidant properties. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A (Terrestrin A) can be used for autoimmune diseases and cancer research.
    Vialinin A
  • HY-160019
    MTX115325
    		Inhibitor
    MTX115325 (Example 1) is an orally active, brain-penetrating USP30 inhibitor (IC50=12 nM) with neuroprotective activity. MTX115325 increases ubiquitination (EC50=32 nM) of the mitochondrial outer membrane protein TOM20 (a USP30 substrate), increasing mitophagy. MTX115325 prevents dopaminergic neuron loss and preserves striatal dopamine.
    MTX115325
  • HY-161378
    UCHL1-IN-1
    		Inhibitor
    UCHL1-IN-1 (Compound 46) is an inhibitor for Ubiquitin C-terminal Hydrolase L1 (UCHL1), with an IC50 of 5.1 μM. UCHL1-IN-1 can be used for cancer research.
    UCHL1-IN-1
  • HY-17543
    ML-323
    		Inhibitor 99.95%
    ML-323 is a reversible, potent USP1-UAF1 inhibitor with IC50 of 76 nM in a Ub-Rho assay. The measured inhibition constants of ML-323 for the free enzyme (Ki) is 68 nM.
    ML-323
  • HY-13817
    IU1
    		Inhibitor 99.42%
    IU1 is a special Usp14 inhibitor with an IC50 of 4-5 μM.
    IU1
  • HY-15667
    P005091
    		Inhibitor 99.92%
    P005091 is a selective and potent inhibitor of ubiquitin-specific protease 7 (USP7) with an EC50 of 4.2 μM.
    P005091
  • HY-13765
    6-Thioguanine
    		Inhibitor 98.01%
    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.
    6-Thioguanine
  • HY-13989
    b-AP15
    		Inhibitor 98.57%
    b-AP15 is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14.
    b-AP15
  • HY-110404
    Capzimin
    		Inhibitor 99.21%
    Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.
    Capzimin
  • HY-18637
    LDN-57444
    		Inhibitor 98.67%
    LDN-57444 is a reversible, competitive and site-directed inhibitor of ubiquitin C-terminal hydrolase L1 (UCH-L1), with an IC50 of 0.88 μM and a Ki of 0.40 μM; LDN-57444 also suppresses UCH-L3 activity, with an IC50 of 25 μM.
    LDN-57444
  • HY-100900
    ML364
    		Inhibitor 99.94%
    ML364 is a selective ubiquitin specific peptidase 2 (USP2) inhibitor (IC50=1.1 μM) with anti-proliferative activity, which direct binds to USP2 (Kd=5.2 μM), induces an increase in cellular cyclin D1 degradation and causes cell cycle arrest. ML364 increases the levels of mitochondrial ROS and decreases in the intracellular content of ATP.
    ML364
  • HY-112438
    MF-094
    		Inhibitor 99.23%
    MF-094 is a potent and selective USP30 inhibitor with an IC50 of 120 nM. MF-094 increases protein ubiquitination and accelerates mitophagy.
    MF-094
  • HY-117370
    USP25/28 inhibitor AZ1
    		Inhibitor ≥98.0%
    USP25/28 inhibitor AZ1 (AZ1) is an orally active, selective, noncompetitive, dual ubiquitin specific protease (USP) 25/28 inhibitor with IC50s of 0.7 μM and 0.6 μM, respectively. USP25/28 inhibitor AZ1 attenuates colitis and tumorigenesis in the mice model.
    USP25/28 inhibitor AZ1
  • HY-50737A
    DUB-IN-2
    		Inhibitor 99.27%
    DUB-IN-2 is a potent deubiquitinase inhibitor with an IC50 of 0.28 μM for USP8.
    DUB-IN-2
  • HY-111458
    GSK2643943A
    		Inhibitor 99.12%
    GSK2643943A is a deubiquitinating enzyme (DUB) inhibitor targeting USP20. GSK2643943A has affinity with an IC50 of 160 nM for USP20/Ub-Rho. GSK2643943A has anti-tumor efficacy and can be used for the research of oral squamous cell carcinoma (OSCC) .
    GSK2643943A
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity