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-18638
    TCID
    		Inhibitor 99.78%
    TCID (4,5,6,7-Tetrachloroindan-1,3-dione) is a potent and selective neuronal ubiquitin C-terminal hydrolase (UCH-L3) inhibitor with an IC50 of 0.6 μM. TCID diminishes glycine transporter GlyT2 ubiquitination in brainstem and spinal cord primary neurons.
    TCID
  • HY-80012
    SJB3-019A
    		Inhibitor 99.88%
    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-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-17540
    HBX 19818
    		Inhibitor 99.25%
    HBX 19818 is a specific inhibitor of ubiquitin-specific protease 7 (USP7), with an IC50 of 28.1 μM.
    HBX 19818
  • 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-12471
    VLX1570
    		Inhibitor 99.95%
    VLX1570 is a competitive inhibitor of proteasome deubiquitinases (DUBs) with an IC50 of approximate 10 μM.
    VLX1570
  • HY-153365
    I-138
    		Inhibitor 99.75%
    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-N6712
    Thiolutin
    		Inhibitor 99.29%
    Thiolutin (Acetopyrrothin) is a sulfur-containing antibiotic, which is a potent inhibitor of bacterial and yeast RNA polymerases. Thiolutin can be produced by Streptomyces. Thiolutin inhibits AMSH (IC50 = 4 μM) and Rpn11 (IC50 = 0.53 μM). Thiolutin is a dual inhibitor of BRCC36 and the NLRP3 inflammasome, exhibiting anti-inflammatory effects. Thiolutin effectively suppresses the interaction between BRCC36 and HMGCR, leading to the inhibition of HCC growth. Thiolutin attenuates pyroptosis and NLRP3 inflammasome activation. Thiolutin markedly alleviates renal injury and inflammatory process in IgAN. Thiolutin is an anti-angiogenic compound which can ease Doxorubicin-induced cardiotoxicity (DOXIC)[1][2][3][4][5].
    Thiolutin
  • HY-15757
    SJB2-043
    		Inhibitor 99.52%
    SJB2-043 is an inhibitor of the native USP1/UAF1 complex with IC50 of 544 nM.
    SJB2-043
  • 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-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-103435
    Vialinin A
    		Inhibitor 99.90%
    Vialinin A (Terrestrin A) is a p-terphenyl compound that can be derived from a Chinese edible mushroom. Vialinin A is an inhibitor of ubiquitin-specific peptidase 4 (USP4) and has anti-inflammatory and antioxidant properties. Vialinin A can alleviate cerebral ischaemia-reperfusion injury-induced neurological deficits and neuronal apoptosis. Vialinin A promotes activation of Keap1-Nrf2-ARE signaling pathway and increases the protein degradation of Keap1. Vialinin A possesses various pharmacological activities in cancer, Kawasaki disease, asthma, and pathological scarring. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A can be studied in reseach for autoimmune diseases, cancer and ischaemic stroke.
    Vialinin A
  • 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-145337
    FT3967385
    		Inhibitor 99.74%
    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-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 can be used in the research of idiopathic pulmonary fibrosis.
    IMP-1710
  • 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-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-136910
    USP7-797
    		Inhibitor 99.09%
    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-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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Deubiquitinase Isoform Comparison

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