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-138995
    IMP-1710
    Inhibitor 99.67%
    IMP-1710 is a potent and selective deubiquitylating enzyme UCHL1 inhibitor with an IC50 value of 38 nM. IMP-1710 has antifibrotic activity. IMP-1710 is a UCHL1 probe to identify and quantify target proteins in intact human cells. IMP-1710 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    IMP-1710
  • 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
  • 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-134817
    USP7-IN-8
    Inhibitor 99.04%
    USP7-IN-8 (example 81) is a selective ubiquitin-specific protease 7 (USP7) inhibitor with an IC50 of 1.4 μM in an Ub-Rho110 assay. USP7-IN-8 shows no activity against USP47 and USP5. USP7-IN-8 has anticancer effects.
    USP7-IN-8
  • HY-12989
    LDN-91946
    Inhibitor 98.70%
    LDN-91946 is a potent, selective and uncompetitive ubiquitin C-terminal hydrolase-L1 (UCH-L1) inhibitor with a Ki app of 2.8 μM.
    LDN-91946
  • HY-158039
    YCH2823
    Inhibitor 99.87%
    YCH2823 is an inhibitor of USP7 (IC50 = 49.6 nM; Kd = 0.117 μM). YCH2823 shows significant efficacy in inhibiting TP53 wild-type and mutant tumors, with approximately 5-fold higher potency than FT671. YCH2823 induce apoptosis. YCH2823 synergistic effects with mTOR inhibitors.
    YCH2823
  • HY-148254
    8RK64
    Inhibitor 99.78%
    8RK64 is a covalent UCHL1 inhibitor (IC50: 0.32 μM). 8RK64 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    8RK64
  • HY-112128
    USP7-IN-3
    Inhibitor 99.06%
    USP7-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.
    USP7-IN-3
  • HY-12988
    C527
    Inhibitor 99.88%
    C527 is a is a pan DUB enzyme inhibitor, with a high potency for the USP1/UAF1 complex (IC50=0.88 μM).
    C527
  • HY-148482
    USP7-IN-11
    Inhibitor 99.31%
    USP7-IN-11 is a potent ubiquitin-specific protease 7 (USP7) (Deubiquitinase) inhibitor with an IC50 of 0.37 nM. USP7-IN-11 has anticancer effects (WO2022048498A1; Example 187).
    USP7-IN-11
  • HY-150505
    DC-U4106
    Inhibitor 99.03%
    DC-U4106 is a USP8 targeting inhibitor with the Kdvalue of 4.7 μM and the IC50 value of 1.2 μM. DC-U4106 can target the ubiquitin pathway and facilitate the degradation of Erα. DC-U4106 inhibits tumor growth with minimal toxicity and has the potential for the research of breast cancer.
    DC-U4106
  • HY-153045A
    BAY-728
    99.92%
    BAY-728 can be used as a negative control of BAY-805. BAY-805 is a potent and selective Inhibitor of USP21.
    BAY-728
  • HY-136528
    RA-9
    Inhibitor 98.67%
    RA-9 is a potent and selective proteasome-associated deubiquitinating enzymes (DUBs) inhibitor with favorable toxicity profile and anticancer activity. RA-9 blocks ubiquitin-dependent protein degradation without impacting 20S proteasome proteolytic activity. RA-9 selectively induces onset of apoptosis in ovarian cancer cell lines and primary cultures derived from donors. RA-9 induces endoplasmic reticulum (ER)-stress responses in ovarian cancer cells.
    RA-9
  • HY-151563A
    OTUB1/USP8-IN-1 TFA
    Inhibitor 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.
    OTUB1/USP8-IN-1 TFA
  • HY-111623
    USP30 inhibitor 11
    Inhibitor 99.81%
    USP30 inhibitor 11 is a selective and potent ubiquitin specific peptidase 30 (USP30) inhibitor with an IC50 of 0.01 μΜ, the example 83 extracted from patent WO2017009650A1. USP30 inhibitor 11 is used for the study of cancer and conditions involving mitochondrial dysfunction.
    USP30 inhibitor 11
  • HY-148099
    USP1-IN-2
    Inhibitor 99.76%
    USP1-IN-2 (Compound I-193) is a potent ubiquitin-specific protease 1 (USP1) inhibitor with an IC50 of less than about 50 nM.
    USP1-IN-2
  • HY-147032
    USP8-IN-1
    Inhibitor 99.07%
    USP8-IN-1 is a USP8 inhibitor with an IC50 of 1.9 μM. USP8-IN-1 inhibits H1975 cell growth with a GI50 of 82.04 μM (CN111138358A; U10).
    USP8-IN-1
  • HY-160768
    OTUB2-IN-1
    Inhibitor 98.79%
    OTUB2-IN-1, a specific inhibitor of OTUB2 (KD: ~12 μM), reduces PD-L1 protein expression in tumor cells and inhibits tumor growth by promoting robust intra-tumor infiltration of cytotoxic T lymphocytes (CTL) .
    OTUB2-IN-1
  • HY-141852
    STAMBP-IN-1
    Inhibitor 98.37%
    STAMBP-IN-1 is a small-molecule inhibitor of STAMBP deubiquitinase, and interrupts STAMBP-Ub-NALP7 interaction. STAMBP-IN-1 decreases protein level of its inflammasome substrate NALP7 and suppresses IL-1b release after Toll-like receptor (TLR) agonism. STAMBP-IN-1 inhibits the activity of STAMBP to cleave recombinant di-Ub with an IC50 value of 0.33 mM.
    STAMBP-IN-1
Cat. No. Product Name / Synonyms Species Source
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