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

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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-12471
    VLX1570
    Inhibitor 99.36%
    VLX1570 is a competitive inhibitor of proteasome deubiquitinases (DUBs) with an IC50 of approximate 10 μM.
    VLX1570
  • HY-D0843S
    N-Ethylmaleimide-d5
    Inhibitor 99.49%
    N-Ethylmaleimide-d5 is the deuterium labeled N-Ethylmaleimide. N-Ethylmaleimide (NEM), a reagent that alkylates free sulfhydryl groups, is a cysteine protease inhibitor[1]. N-ethylmaleimide specific inhibits phosphate transport in mitochondria[2]. N-Ethylmaleimide is also a deubiquitinating enzyme inhibitor[3].
    N-Ethylmaleimide-d<sub>5</sub>
  • HY-80012
    SJB3-019A
    Inhibitor 99.68%
    SJB3-019A is a potent and novel USP1 inhibitor, 5 times more potent than SJB2-043 in promoting ID1 degradation and cytoxicity in K562 cells with IC50 of 0.0781 μM.
    SJB3-019A
  • HY-103435
    Vialinin A
    Inhibitor 99.89%
    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-122885
    IU1-248
    Inhibitor 99.19%
    IU1-248, a derivative of IU1, is a potent and selective USP14 inhibitor with an IC50 of 0.83?μM.
    IU1-248
  • HY-160019
    MTX115325
    Inhibitor 99.08%
    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-101666
    HBX 41108
    Inhibitor 99.61%
    HBX 41108 is an inhibitor of ubiquitin-specific protease 7 (USP7) with an IC50 of 424 nM. HBX 41108 inhibits USP7-mediated p53 deubiquitination to stabilize p53 and inhibits cancer cell growth. BX 41108 can be used in cancer and diabetes research.
    HBX 41108
  • HY-153365
    I-138
    Inhibitor 99.88%
    I-138 is an orally active, reversible inhibitor of USP1-UAF1 (IC50: 4.1 nM; Ki: 5.4 nM), structurally related to ML323 (HY-17543). I-138 induces monoubiquitination of FANCD2 and PCNA in cells and eliminates USP1 autocleavage in cells.
    I-138
  • HY-13487
    USP7/USP47 inhibitor
    Inhibitor 98.63%
    USP7/USP47 inhibitor is a selective ubiquitin-specific protease 7/47 (USP7/USP47) inhibitor, with EC50s of 0.42 μM and 1.0 μM, respectively.
    USP7/USP47 inhibitor
  • HY-15757
    SJB2-043
    Inhibitor 98.06%
    SJB2-043 is an inhibitor of the native USP1/UAF1 complex with IC50 of 544 nM.
    SJB2-043
  • HY-145337
    FT3967385
    Inhibitor 99.93%
    FT3967385 is a novel USP30 inhibitor that recapitulates genetic loss of USP30 and sets the trigger for PINK1-PARKIN amplification of mitochondrial ubiquitylation.
    FT3967385
  • HY-143345
    EN523
    98.99%
    EN523 is a OTUB1 recruiter. EN523 targets a non-catalytic allosteric cysteine C23 in the K48-ubiquitin-specific deubiquitinase OTUB1.
    EN523
  • HY-100708
    NSC632839
    Inhibitor 98.87%
    NSC632839 is a nonselective isopeptidase inhibitor, which inhibits USP2, USP7, and SENP2 with EC50s of 45±4 μM, 37±1 μM, and 9.8±1.8 μM, respectively.
    NSC632839
  • HY-50737
    DUB-IN-3
    Inhibitor 98.41%
    DUB-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.
    DUB-IN-3
  • HY-149230
    USP28-IN-4
    Inhibitor 99.35%
    USP28-IN-4 is a USP28 inhibitor (IC50=0.04 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-4 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-4 also decreases the ankyrase-1/2 level in vitro. USP28-IN-4 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331).
    USP28-IN-4
  • HY-146887
    USP7-IN-9
    Inhibitor 98.10%
    USP7-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.
    USP7-IN-9
  • HY-160700
    TNG348
    Inhibitor 99.74%
    TNG348 is an orally active ubiquitin-specific protease USP1 inhibitor that can be used in research on cancers with BRCA1/2 mutations or HRD+ (Homologous Recombination Deficiency positive) status.
    TNG348
  • HY-148369
    U7D-1
    Inhibitor 99.65%
    U7D-1 is a first-in-class potent and selective USP7 (ubiquitin-specific protease 7) PROTAC degrader, with a DC50 of 33 nM in RS4;11 cells. U7D-1 shows anticancer activity. U7D-1 induces apoptosis in Jeko-1 cells.
    U7D-1
  • HY-153627
    GK13S
    Inhibitor ≥98.0%
    G13KS is a deubiquitinase UCHL1 ligand and inhibitor. G13KS inhibits recombinant and cellular UCHL1. G13KS reduces levels of monoubiquitin in human glioblastoma cells. GK13S is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    GK13S
  • HY-50736
    DUB-IN-1
    Inhibitor 99.79%
    DUB-IN-1 is an active inhibitor of ubiquitin-specific proteases (USPs), with an IC50 of 0.85 μM for USP8.
    DUB-IN-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity

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