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.

Deubiquitinase Isoform Specific Products:

Deubiquitinase Isoform Comparison
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-D0843
    N-Ethylmaleimide
    		Inhibitor 99.89%
    N-Ethylmaleimide (NEM) derives from maleic acid, it can alkylates free sulfhydryl. N-Ethylmaleimide is an irreversible cysteine protease inhibitor. N-ethylmaleimide specific inhibits phosphate transport in mitochondria. N-Ethylmaleimide inhibits prolyl endopeptidase with an IC50 value of 6.3 μM. N-Ethylmaleimide can be used to modify cysteine residues in proteins and peptides.
    N-Ethylmaleimide
  • 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 99.54%
    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-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-178500A
    WCY-8-67 TFA
    		Inhibitor 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.
    WCY-8-67 TFA
  • HY-180561
    WWQ-03-012
    		Inhibitor 98.04%
    WWQ-03-012 is a selective deSUMOylating isopeptidases DESI2 inhibitor with an IC50 of 47.3 μM. WWQ-03-012 cans induce JAK2-V617F ubiquitination-proteasome degradation with no significant effect on wild-type JAK2. WWQ-03-012 can block JAK2-STAT3/5 signaling, inhibit cell proliferation and induce apoptosis. WWQ-03-012 has a synergistic effect in combination with Ruxolitinib (HY-50856), further enhancing its killing effect on JAK2 mutant cells. WWQ-03-012 can be used for the research of cancer, such as myeloproliferative neoplasms.
    WWQ-03-012
  • HY-179630
    MS102
    		Inhibitor
    MS102 is an orally active ubiquitin specific peptidase 2 (USP2) inhibitor with an IC50 of 5.46 μM. MS102 has viable antiviral activity against ACE2-dependent coronaviruses. MS102 significantly reduces V-domain Ig suppressor of T cell activation (VISTA) protein abundance in vitro and in vivo. MS102 can be used for the study of SARS-CoV-2. MS102 can be used in combination with anti-PD-1 immunotherapy to enhance the anti-tumor immune response.
    MS102
  • HY-13765
    6-Thioguanine
    		Inhibitor 99.54%
    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-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-13817
    IU1
    		Inhibitor 99.30%
    IU1 is a selective, reversible USP14 inhibitor with an IC50 of 4-5 μM. IU1 binds USP14’s catalytic cleft to block deubiquitinase activity. IU1 induces calpain-dependent Tau cleavage, causes ATP deficits, reduces E1~Ub thioester levels and 26S proteasome assembly. IU1 enhances 26S proteasome chymotrypsin-like activity, modulates LC3B-dependent autophagy flux, reduces cancer cell proliferation and migration, and blocks G0/G1 to S phase cell cycle transition in follicular thyroid cancer cells. IU1 activates autophagy-lysosomal and ubiquitin-proteasome pathways, triggers apoptosis, and reduces cervical cancer cell growth. IU1 enhances degradation of proteasome substrates linked to neurodegenerative disease, accelerates oxidized protein degradation, and increases oxidative stress resistance. IU1 can be used for the research of Alzheimer’s disease, follicular thyroid cancer, ischemic stroke, cervical cancer, and neurodegenerative disease.
    IU1
  • HY-17543
    ML-323
    		Inhibitor 99.51%
    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-100900
    ML364
    		Inhibitor 99.96%
    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-18637
    LDN-57444
    		Inhibitor 98.93%
    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-112134
    CSN5i-3
    		Inhibitor 99.95%
    CSN5i-3 is a potent, selective and orally available inhibitor of CSN5/Jab1, and inhibits CSN-catalysed Cul1 deneddylation with an IC50 value of 5.8 nM.
    CSN5i-3
  • HY-145471
    KSQ-4279
    		Inhibitor 99.96%
    KSQ-4279 (USP1-IN-1) is a potent USP1 inhibitor and a selective PARP1 inhibitor. KSQ-4279 is promising for research of cancers.
    KSQ-4279
  • HY-110404
    Capzimin
    		Inhibitor 99.19%
    Capzimin is a potent and moderately specific proteasome isopeptidase Rpn11 inhibitor.
    Capzimin
  • HY-112438
    MF-094
    		Inhibitor 99.75%
    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-13989
    b-AP15
    		Inhibitor 98.05%
    b-AP15 is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14.
    b-AP15
  • HY-50737A
    DUB-IN-2
    		Inhibitor 99.92%
    DUB-IN-2 is a potent deubiquitinase inhibitor with an IC50 of 0.28 μM for USP8.
    DUB-IN-2
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Deubiquitinase Isoform Comparison

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