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-156525
    USP1-IN-6
    		Inhibitor
    USP1-IN-6 (compound 11) is a USP1 inhibitor (IC50<50 nM). USP1-IN-5 also inhibits MDA-MB-436 cells with IC50 <50 nM.
    USP1-IN-6
  • HY-P10416
    Q14
    		Inhibitor
    Q14 is a polypeptide derived from the USP30 (ubiquitin specific peptidase 30) transmembrane (TM) domain with the ability to inhibit the deubiquitination activity of USP30 (IC50=57.2 nM). Q14 reduces USP30 activity by inhibiting the interaction between the USP30 transmembrane domain and its catalytic domain. Q14 peptide contains the LC3 interaction region (LIR) motif, which enables it to bind to the LC3 and accelerate the formation of autophagosomes, thereby promoting mitophagy. Q14 can be used in the study of neurodegenerative diseases as well as mitochondrial quality control and cell metabolism.
    Q14
  • HY-P10800
    T20-M
    T20-M is a lead peptide that shows good potential for binding affinity towards UBE2C.
    T20-M
  • HY-153996
    CT1113
    		Inhibitor
    CT1113 is a potent USP28 and USP25 inhibitor. CT1113 decreases the MYC level in vivo，exhibits anti-tumor activity in mouse pancreatic cancer CDX model.
    CT1113
  • HY-168267
    XH161-180
    		Inhibitor
    XH161-180 is a potent and orally active ubiquitin carboxyl-terminal hydrolase 2 (USP2) inhibitor. XH161-180 decreases the protein of cyclin D and ACE2. XH161-180 shows antiproliferative activity. XH161-180 has the potential for the research of cancer and virus infection depending on ACE2.
    XH161-180
  • HY-153942
    USP7-IN-12
    		Inhibitor
    USP7-IN-12 (compound 1) is a potent and orally active Usp7 inhibitor with an IC50 value of 3.67 nM. USP7-IN-12 shows antiproliferative activity.
    USP7-IN-12
  • HY-161878
    USP1-IN-10
    		Inhibitor
    USP1-IN-10 (compound 2) is a potent tricyclic USP1 inhibitor with an IC50 of 7.6 nM. USP1-IN-10 inhibits MDA-MB-436 viability (IC50=21.58 nM). USP1-IN-10 has the potential for cancers research.
    USP1-IN-10
  • HY-168266
    MS1172
    		Inhibitor
    MS1172 (XH161-172; Example 54) is an orally active and potent inhibitor of USP2. MS1172 plays an important role in cancer and virus infection.
    MS1172
  • HY-160515
    USP7-IN-13
    		Inhibitor
    USP7-IN-13 (Compound 101) is a USP7 inhibitor with an IC50 value of 0.2-1 μM, which can be used for the study of multiple myeloma.
    USP7-IN-13
  • 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-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-145471A
    KSQ-4279 (gentisate)
    		Inhibitor
    KSQ-4279 (gentisate) (Compound Formula I) is a potent USP1 inhibitor and a selective PARP1 inhibitor. KSQ-4279 (gentisate) is promising for research of cancers.
    KSQ-4279 (gentisate)
  • 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-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-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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity
Deubiquitinase Isoform Comparison

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