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-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-12471
    VLX1570
    		Inhibitor 99.95%
    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-103435
    Vialinin A
    		Inhibitor 99.90%
    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-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-80012
    SJB3-019A
    		Inhibitor 99.82%
    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-13487
    USP7/USP47 inhibitor
    		Inhibitor 98.58%
    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-112937
    GNE-6640
    		Inhibitor 99.91%
    GNE-6640 is a selective and non-covalent inhibitor of ubiquitin epecific peptidase 7 (USP7), with IC50 values of 0.75 μM, 0.43 μM, 20.3 μM and 0.23 μM for full length USP7, USP7 catalytic domain, full length USP47 and Ub-MDM2, respectively.
    GNE-6640
  • 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-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-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-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-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-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
    		Ligand 99.22%
    EN523 is a OTUB1 recruiter. EN523 targets a non-catalytic allosteric cysteine C23 in the K48-ubiquitin-specific deubiquitinase OTUB1.
    EN523
  • HY-160700
    TNG348
    		Inhibitor 99.74%
    TNG348 is an orally available allosteric inhibitor of the ubiquitin-specific protease USP1. TNG348 specifically and efficiently inhibits the activity of USP1, inhibiting its deubiquitination of proliferative PCNA and FANCD2, thereby disrupting the DNA repair process. TNG348 has inhibitory activity against breast and ovarian cancers carrying BRCA1/2 mutations and other homologous recombination defects (HRD) .
    TNG348
  • 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-122883
    BC-1471
    		Inhibitor 99.69%
    BC-1471 is a STAM-binding protein (STAMBP) deubiquitinase inhibitor. BC-1471 inhibits NALP7 (NACHT, LRR and PYD domains-containing protein 7) inflammasome activity.
    BC-1471
  • HY-136910
    USP7-797
    		Inhibitor
    USP7-797 (USP7-IN-7) is an orally available, selective USP7 inhibitor (IC50=0.5 nmol/L) with antitumor activity. USP7-797 reduces the level of MDM2, thereby increasing the stability and activity of p53, leading to cell cycle arrest and apoptosis. USP7-797 has low nanomolar cytotoxicity against p53 mutant cancer cell lines, p53 wild-type hematological tumors, and neuroblastoma cell lines.
    USP7-797
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Deubiquitinase Isoform Comparison

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