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-D2188
    IMP-2373
    		Chemical
    IMP-2373 is the activity-based probe (ABP). IMP-2373 is a covalent pan- deubiquitinase(DUB) ABP to monitor DUB activity in physiologically relevant live cells.
    IMP-2373
  • HY-168220
    FX-171-C
    		Inhibitor
    FX-171-C is a noncompetitive Deubiquitinase inhibitor with an IC50 of 1.4 µM.
    FX-171-C
  • HY-141659A
    (R)-CMPD-39
    		99.78%
    (R)-CMPD-39 is the R enantiomer of CMPD-39 ( HY-141659 ). CMPD-39 is a selective non-covalent inhibitor of the ubiquitin-specific protease USP30 (IC50 =~20 nM), with high selectivity over other DUB family members (1-100 μM). CMPD-39 inhibits the deubiquitinating activity of USP30, enhances the ubiquitination of mitochondrial proteins TOMM20 and SYNJ2BP; thus, CMPD-39 promotes phosphoubuitin accumulation, thereby accelerating mitochondrial autophagy (mitophagy) and peroxisomal autophagy (pexophagy). CMPD-39 significantly restores impaired mitochondrial function in dopaminergic neurons derived from Parkinson's disease patients.
    (R)-CMPD-39
  • HY-176703
    USP1-IN-12
    		Inhibitor
    USP1-IN-12 (compound 4) is a potent and orally activeUSP1 inhibitor with an IC50 value of 0.00366 µM. USP1-IN-12 inhibits cell clone formation.
    USP1-IN-12
  • HY-161447
    USP1-IN-8
    		Inhibitor
    USP1-IN-8 (Compound 16) is an inhibitor for ubiquitin specific peptidase 1 (USP1) and its cofactor UAF1, with IC50 ≤50 nM. USP1-IN-8 inhibits proliferation of MDA-MB-436 with IC50 ≤50 nM.
    USP1-IN-8
  • HY-172824
    MS7131
    MS7131 is a USP1-recruiting DUBTACs. MS7131 effectively reduces histone H3 lysine 27 trimethylation and significantly suppresses the proliferation and clonogenicity of cancer cells.
    MS7131
  • HY-122646
    USP7-IN-2
    		Inhibitor
    USP7-IN-2 (compound 4) is a non-competitive USP7 inhibitor with an IC50 of 6 nM. USP7-IN-2 causes degradation of MDM2, stabilization of p53 and induction of p21 in multiple cell lines, and can be utilized in cancer research.
    USP7-IN-2
  • HY-172220
    ChlaDUB1-IN-2
    		Inhibitor
    ChlaDUB1-IN-2 (Compound 27a) is the inhibitor for Chlamydia trachomatis deubiquitinase ChlaDUB1 with an IC50 of 0.97 μM. ChlaDUB1-IN-2 inhibits the inclusion body formation of C. trachomatis with an IIC50 of 25.6 μg/mL.
    ChlaDUB1-IN-2
  • HY-176426
    Subquinocin
    		Inhibitor
    Subquinocin is a CYLD inhibitor that inhibits USP family deubiquitinases (DUBs). Subquinocin enhances the activation of NF-κB and IFN pathways by inhibiting CYLD. Subquinocin promotes RIG-I-mediated activation of IRF3 and/or IRF7 in the interferon pathway.
    Subquinocin
  • HY-161909
    USP30-I-1
    		Inhibitor
    USP30-I-1 is a selective inhibitor of USP30 with an IC50 value of 94 nM. USP30-I-1 can be used in the research of diseases with impaired mitophagy by targeting USP30.
    USP30-I-1
  • HY-D0843R
    N-Ethylmaleimide (Standard)
    		Inhibitor
    Bayogenin (Standard) is the analytical standard of Bayogenin. This product is intended for research and analytical applications. Bayogenin is an alfalfa saponin, shows moderate potency of glycogen phosphorylase inhibition.
    N-Ethylmaleimide (Standard)
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Deubiquitinase Isoform Comparison

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