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-D1726
    8RK59
    		Inhibitor
    8RK59, a Bodipy probe, is a potent UCHL1 (ubiquitin C-terminal hydrolase L1) inhibitor, with an IC50 close to 1 μM. 8RK59 could penetrate and label living cells. BodipyFL-alkyne is coupled to the azide of 8RK64 (HY-148254) using copper(I)-mediated click chemistry, resulting in compound 8RK59.
    8RK59
  • HY-159964
    USP7-IN-16
    		Inhibitor
    USP7-IN-16 (Compound 61) is a selective USP7 inhibitor with IC50 values of 5.5 nM in the FLINT assay and 2.1 nM in MM.1S cells. USP7-IN-16 exhibits antitumor activity in mice and is a promising candidate for research in the field of oncology.
    USP7-IN-16
  • HY-149228
    USP28-IN-2
    		Inhibitor
    USP28-IN-2 is a USP28 inhibitor (IC50=0.3 μM) with high selectivity over USP2, USP7, USP8, USP9x, UCHL3 and UCHL5. USP28-IN-2 shows cytotoxicity against cancer cells, down-regulates the cellular level of c-Myc through ubiquitin-proteasome system. USP28-IN-2 also decreases the ankyrase-1/2 level in vitro. USP28-IN-2 enhance the sensitivity of colorectal cancer cells to Regorafenib (HY-10331).
    USP28-IN-2
  • HY-173352
    USP7 activator 1
    USP7 activator 1 (compound MS-8) is an activator of USP7 by engaging the allosteric C-terminal binding pocket of USP7.
    USP7 activator 1
  • HY-156524
    USP1-IN-5
    		Inhibitor
    USP1-IN-5 (compound 10) is a USP1 inhibitor (IC50<50 nM). USP1-IN-5 also inhibits MDA-MB-436 cells with IC50 <50 nM.
    USP1-IN-5
  • HY-163769
    DUB-IN-8
    		Inhibitor
    DUB-IN-8 (Compound 8q) is an inhibitor for Chlamydia deubiquitinase 1 (DUB1), with IC50 of 7.7 μM. DUB-IN-8 exhibits antimicrobial activity, inhibits the chlamydial inclusions with an IIC50 (the concentration to induce 50% inclusion inhibition) of 8.5 μg/mL.
    DUB-IN-8
  • HY-162794
    YCH3124
    		Inhibitor
    YCH3124 (compound Z33) is a USP7 inhibitor (IC50=41.9 nM) with antitumor activity. YCH3124 has good in vitro antiproliferative activity against various tumor cells including LNCaP (IC50=3.6 nM) and CHP-212 (IC50=9.9 nM). In addition, YCH3124 disrupts cell cycle progression by restricting G1 phase and induces apoptosis in CHP-212 cells.
    YCH3124
  • HY-162633
    USP1-IN-9
    USP1-IN-9 (Compound 1m) is reversible and noncompetitive ubiquitin-specific proteases (USP1) inhibitors with an IC50 of 8.8 nM, which is designed and synthesized to pyrido[2,3-d]pyrimidin-7(8H)-one derivative based on the disclosed structure of ML323(HY-17543) and KSQ-4279(HY-145471). USP1-IN-9 displays excellent USP1/UAF inhibition and exhibits strong antiproliferation effect in breast cancer cells. USP1-IN-9 can generate enhanced cell killing with PARP inhibitor olaparib(HY-10162) in olaparib-resistant MDA-MB-436/OP cells, which is promising for research in the field of cancer.
    USP1-IN-9
  • HY-159175
    XM-U-14
    		Degrader
    XM-U-14 is a selective PROTAC USP7 Degrader (DC50: 0.74 nM in inducing USP7 degradation in RS4;11 cell line). XM-U-14 upregulates the levels of p53 and p21. XM-U-14 also significantly inhibits acute lymphoblastic leukemia (ALL) cell growth (IC50: 0.5 nM and 8.3 nM for RS4;11 cells and Reh cells respectively). XM-U-14 induces apoptosis and cycle arrest. XM-U-14 inhibits tumor growth. (Blue: VHL ligand (HY-159465), Black: linker (HY-W539783); Pink: USP7 inhibitor (HY-159464)).
    XM-U-14
  • HY-156001
    DUB-IN-7
    		Inhibitor
    DUB-IN-7 (compound 43) is a Deubiquitinating enzymes (DUBs) inhibitor. DUB-IN-7 can be used in the study of diseases mediated by dysregulated JAK2 activity, such as leukemia.
    DUB-IN-7
  • HY-153731
    USP1-IN-4
    		Inhibitor
    USP1-IN-4 (compound 10) is an effective USP1 inhibitor with an IC50 value of 2.44 nM. USP1-IN-4 has anticancer activity and synergistic activity with various anticancer drugs.
    USP1-IN-4
  • HY-168121
    USP7-IN-15
    		Inhibitor
    USP7-IN-15 (compound J21) is a USP7 inhibitor, with an IC50 of 41.35 nM.
    USP7-IN-15
  • HY-172193
    UBD1031
    		Ligand
    UBD1031 exhibits good affinity to the ubiquitin binding domain (UBD) of USP16 with a KD of 48 nM. UBD1031 inhibits the interaction between USP16 and ISG15 with an EC50 of 1.7 nM. UBD1031 can be used a chemical probe for USP16 UBD.
    UBD1031
  • HY-N6712R
    Thiolutin (Standard)
    		Inhibitor
    Erythromycin (Standard) is the analytical standard of Erythromycin. This product is intended for research and analytical applications. Erythromycin is a macrolide antibiotic produced by actinomycete?Streptomyces erythreus?with a broad spectrum of antimicrobial activity. Erythromycin binds to bacterial 50S ribosomal subunits and inhibits?RNA-dependent protein synthesis?by blockage of transpeptidation and/or translocation reactions, without affecting synthesis of nucleic acid. Erythromycin also exhibits antitumor and neuroprotective effect in different fields of research.
    Thiolutin (Standard)
  • HY-111166
    USP7/USP47 inhibitor 1
    		Inhibitor
    USP7/USP47 inhibitor 1 (compound 2) is an inhibitor of USP47, with an EC50 of 14 μM. USP7/USP47 inhibitor 1 has an EC50 of >31.6 μM for USP7. USP7/USP47 inhibitor 1 can be used for cancer research.
    USP7/USP47 inhibitor 1
  • HY-164544
    USP7-055
    		Inhibitor
    USP7-055 is a USP7 inhibitor. USP7-055 can be used in cancer research.
    USP7-055
  • HY-124739
    HBX 28258
    		Inhibitor
    HBX 28258 is a selective USP7 inhibitor, with an IC50 of 22.6 μM. HBX 28258 can covalently binds to Cys223 located in the catalytic core of USP7, inhibits its deubiquitinating activity, promotes MDM2 protein degradation, and activates p53.
    HBX 28258
  • HY-15432
    (E/Z)-NSC-687852
    (E/Z)-NSC-687852 is a isomer of NSC-687852 (HY-13989). NSC687852 (b-AP15) is a specific inhibitor of the deubiquitinating enzymes UCHL5 and Usp14.
    (E/Z)-NSC-687852
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Deubiquitinase Isoform Comparison

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