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Deubiquitinase inhibitor

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Art. -Nr. Produktname Target Forschungsgebiete Chemical Structure
  • HY-50737A
    DUB-IN-2
    15+ Cited Publications

    		 Deubiquitinase Cancer
    DUB-IN-2 is a potent deubiquitinase inhibitor with an IC50 of 0.28 μM for USP8 .
    DUB-IN-2
  • HY-13817
    IU1
    Maximum Cited Publications
    25 Publications Verification

    		 Deubiquitinase Autophagy Apoptosis Cardiovascular Disease Neurological Disease Endocrinology Cancer
    IU1 is a selective, reversible USP14 inhibitor with an IC50 of 4-5 μM. IU1 binds USP14’s catalytic cleft to block deubiquitinase activity. IU1 induces calpain-dependent Tau cleavage, causes ATP deficits, reduces E1~Ub thioester levels and 26S proteasome assembly. IU1 enhances 26S proteasome chymotrypsin-like activity, modulates LC3B-dependent autophagy flux, reduces cancer cell proliferation and migration, and blocks G0/G1 to S phase cell cycle transition in follicular thyroid cancer cells. IU1 activates autophagy-lysosomal and ubiquitin-proteasome pathways, triggers apoptosis, and reduces cervical cancer cell growth. IU1 enhances degradation of proteasome substrates linked to neurodegenerative disease, accelerates oxidized protein degradation, and increases oxidative stress resistance. IU1 can be used for the research of Alzheimer’s disease, follicular thyroid cancer, ischemic stroke, cervical cancer, and neurodegenerative disease .
    IU1
  • HY-13264
    Degrasyn
    15+ Cited Publications

    WP1130

    		 Deubiquitinase Bcr-Abl Autophagy Apoptosis Cancer
    Degrasyn (WP1130) is a cell-permeable deubiquitinase (DUB) inhibitor, directly inhibiting DUB activity of USP9x, USP5, USP14, and UCH37. Degrasyn has been shown to downregulate the antiapoptotic proteins Bcr-Abl and JAK2.
    Degrasyn
  • HY-138794
    XL177A
    5 Publications Verification

    		 Deubiquitinase Histone Demethylase SARS-CoV Cancer
    XL177A is a covalent USP7 inhibitor that blocks the deubiquitinase activity of USP7. XL177A destabilizes non-canonical PRC1 complexes or KDM6A and reduces chromatin deposition of H2AK119Ub, thereby relieving the repression of neuronal differentiation programs. Meanwhile, XL177A also regulates the ELOF1-UVSSA-USP7-nuclear β-catenin axis, decreasing the transcription levels of related proteins and the accumulation of nuclear β-catenin. XL177A exerts antiviral effects by reducing the expression levels of coronavirus receptors, and exhibits inhibitory activity against APC-mutated colorectal cancer cells, neuroblastoma, and coronaviruses including SARS-CoV-2 variants. XL177A is mainly used in studies related to colorectal cancer, neuroblastoma, and coronavirus infections .
    XL177A
  • HY-111408
    EOAI3402143
    10+ Cited Publications

    		 Deubiquitinase Cancer
    EOAI3402143 is a deubiquitinase (DUB) inhibitor, which inhibits dose-dependently inhibits Usp9x/Usp24 and Usp5.
    EOAI3402143
  • HY-12471
    VLX1570
    2 Publications Verification

    		 Deubiquitinase Cancer
    VLX1570 is a competitive inhibitor of proteasome deubiquitinases (DUBs) with an IC50 of approximate 10 μM.
    VLX1570
  • HY-176426
    Subquinocin

    		Deubiquitinase NF-κB IFNAR Cancer
    Subquinocin is a tumor suppressor CYLD inhibitor that inhibits USP family deubiquitinases (DUBs) activity of CYLD with an IC50 of 30 μM. Subquinocin enhances the activation of NF-κB and IFN pathways by inhibiting CYLD. Subquinocin promotes RIG-I-mediated activation of IRF3/IRF7 in the interferon pathway. Subquinocin can be used for the research of cancer and neurodegenerative diseases .
    Subquinocin
  • HY-N0886
    Aloin B
    3 Publications Verification

    Isobarbaloin

    		 SARS-CoV Virus Protease Infection Endocrinology Cancer
    Aloin B (Isobarbaloin) is an orally active SARS-CoV-2 papain-like protease (PLpro) inhibitor with an IC50 of 16.08 μM (hydrolytic activity) and 17.51 μM (deubiquitinase activity). Aloin B is metabolized by rat intestinal flora into aloe-emodin-9-anthrone to exert laxative effects. Aloin B inhibits TPA (HY-18739)-induced ear edema, putrescine elevation, and tumor promotion in mouse skin. Aloin B can be used in research related to anti-inflammation, tumor promotion inhibition, coronavirus disease 2019 (COVID-19) and constipation .
    Aloin B
  • HY-145337
    FT3967385

    FT385

    		 Deubiquitinase PINK1/Parkin Neurological Disease Cancer
    FT3967385 (FT385) is a selective covalent inhibitor that targets the outer mitochondrial membrane deubiquitinase (Deubiquitinase) USP30 (IC50 = 1.5 nM, Ki = 0.014 μM). By inhibiting the enzymatic activity of USP30, FT3967385 relieves its negative regulation of the PINK1-Parkin mediated mitochondrial ubiquitination cascade, thereby enhancing mitophagy. FT3967385 can be used for mechanistic studies of neurodegenerative diseases associated with mitochondrial dysfunction, such as Parkinson's disease .
    FT3967385
  • HY-153627
    GK13S

    		Deubiquitinase Cancer
    GK13S is a deubiquitinase UCHL1 ligand and inhibitor. GK13S inhibits recombinant and cellular UCHL1. GK13S 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-141852
    STAMBP-IN-1

    		Deubiquitinase Inflammation/Immunology
    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
  • HY-122883
    BC-1471
    1 Publications Verification

    		 Deubiquitinase Interleukin Related Caspase Inflammation/Immunology
    BC-1471 is a STAMBP deubiquitinase inhibitor with an IC50 of 0.33 μM. BC-1471 can inhibit the activity of the NALP7 inflammasome. BC-1471 has anti-inflammatory activity and can be used for the research of inflammatory diseases .
    BC-1471
  • HY-148482
    USP7-IN-11

    		Deubiquitinase Cancer
    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-138978
    MF-095

    		Mitophagy Deubiquitinase Neurological Disease
    MF-095 is a USP30 inhibitor. MF-095 promotes mitochondrial autophagy. MF-095 can be used in neurological disease-related research .
    MF-095
  • HY-120458
    LCAHA
    1 Publications Verification

    LCA hydroxyamide

    		 Deubiquitinase Cancer
    LCAHA (LCA hydroxyamide) is a deubiquitinase USP2a inhibitor with IC50s of 9.7 μM and 3.7μM in Ub-AMC Assay and Di-Ub Assay, respectively. LCAHA destabilizes Cyclin D1 and induces G0/G1 arrest by inhibiting deubiquitinase USP2a .
    LCAHA
  • HY-149902
    USP8-IN-3

    		Deubiquitinase Cancer
    USP8-IN-3 (Compd U51) is a deubiquitinase USP8 inhibitor with an IC50 value of 4.0 μM. USP8-IN-3 also inhibits the proliferation of GH3 and H1957 cells with GI50s of 37.03 μM and 6.01 μM, respectively .
    USP8-IN-3
  • HY-149901
    USP8-IN-2

    		Deubiquitinase Cancer
    USP8-IN-2 (Compd U52) is a deubiquitinase USP8 inhibitor with an IC50 value of 6.0 μM. USP8-IN-2 also inhibits the proliferation of H1957 cells with an GI50 value of 24.93 μM, respectively .
    USP8-IN-2
  • HY-114383
    ST-539

    		Deubiquitinase Autophagy Neurological Disease
    ST-539 is the inhibitor for deubiquitinase USP30 with IC50 of 0.37 μM. ST-539 promotes the ubiquitination of mitochondrial proteins, and induces mitochondrial autophagy, thereby regulating mitochondrial homeostasis. ST-539 can be used in research of neurodegenerative diseases .
    ST-539
  • HY-124855
    STD1T
    1 Publications Verification

    		 Deubiquitinase Cancer
    STD1T is a deubiquitinase USP2a inhibitor with an IC50 of 3.3 μM in Ub-AMC Assay .
    STD1T
  • HY-138794A
    (Rac)-XL177A

    		Deubiquitinase Cancer
    (Rac)-XL177A is the racemic isomer of XL177A (HY-138794). XL177A is a covalent USP7 inhibitor that blocks the deubiquitinase activity of USP7. XL177A destabilizes non-canonical PRC1 complexes or KDM6A and reduces chromatin deposition of H2AK119Ub, thereby relieving the repression of neuronal differentiation programs. Meanwhile, XL177A also regulates the ELOF1-UVSSA-USP7-nuclear β-catenin axis, decreasing the transcription levels of related proteins and the accumulation of nuclear β-catenin. XL177A exerts antiviral effects by reducing the expression levels of coronavirus receptors, and exhibits inhibitory activity against APC-mutated colorectal cancer cells, neuroblastoma, and coronaviruses including SARS-CoV-2 variants. XL177A is mainly used in studies related to colorectal cancer, neuroblastoma, and coronavirus infections .
    (Rac)-XL177A
  • HY-172220
    ChlaDUB1-IN-2

    		Deubiquitinase Bacterial Infection
    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-158774
    TG2-179-1

    		Apoptosis Cancer
    TG2-179-1 is a potent BAP1 inhibitor. TG2-179-1 inhibits the domain-containing deubiquitinase (DUB) activity of BAP1 by covalently binding to its active site. TG2-179-1 exerts cytotoxic activity, leading to defective replication and increased apoptosis. TG2-179-1 has the potential for colon cancer research .
    TG2-179-1
  • HY-174301
    USP7-IN-18

    		Deubiquitinase DNA Methyltransferase MDM-2/p53 Cancer
    USP7-IN-18 is a naphthalene derivative. USP7-IN-18 is a selective USP7 inhibitor (IC50 : 130.9 nM), with no or very weak inhibition of the other 8 DUBs including USP47. USP7-IN-18 specifically binds to the catalytic domain of USP7, blocking its deubiquitinase activity. USP7-IN-18 causes degradation of the oncogenic proteins MDM2 and DNMT1, and also degrades the novel target PCLAF. USP7-IN-18 activates the p53-p21 pathway. USP7-IN-18 exerts anti-tumor effects in colon cancer animal models and reshapes the tumor immune microenvironment. USP7-IN-18 achieves both direct cytotoxic and immune-synergistic anti-tumor actions.
    USP7-IN-18
  • HY-168220
    FX-171-C

    		Deubiquitinase Cancer
    FX-171-C is a noncompetitive Deubiquitinase inhibitor with an IC50 of 1.4 µM .
    FX-171-C
  • HY-169154
    ChlaDUB1-IN-1

    		Bacterial Infection
    ChlaDUB1-IN-1 (Compound 8) is an inhibitor for Chlamydia deubiquitinase 1 (ChlaDUB1). ChlaDUB1-IN-1 can be used in antimicrobial research .
    ChlaDUB1-IN-1
  • HY-164689
    Cadmium pyrithione

    		Proteasome Cancer
    Cadmium pyrithione is a metal compound that inhibits protein deubiquitinase activity. Cadmium pyrithione treatment results in significant accumulation of ubiquitinated proteins in cancer cells and primary leukemia cells. Cadmium pyrithione strongly inhibits the activity of proteasome deubiquitinase (such as USP14 and UCHL5), but has a smaller inhibitory effect on 20S proteasome activity. The anticancer activity of Cadmium pyrithione is associated with the induction of apoptosis through caspase activation. Furthermore, Cadmium pyrithione inhibition inhibited proteasome function and suppressed tumor growth in animal xenograft models .
    Cadmium pyrithione
  • HY-163769
    DUB-IN-8

    		Deubiquitinase Bacterial Infection
    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-N0886R
    Aloin B (Standard)

    Isobarbaloin (Standard)

    		 Reference Standards Virus Protease SARS-CoV Infection Metabolic Disease Cancer
    Aloin B (Isobarbaloin) (Standard) is the analytical standard of Aloin B. This product is intended for research and analytical applications. Aloin B is an orally active SARS-CoV-2 papain-like protease (PLpro) inhibitor with an IC50 of 16.08 μM (hydrolytic activity) and 17.51 μM (deubiquitinase activity). Aloin B is metabolized by rat intestinal flora into aloe-emodin-9-anthrone to exert laxative effects. Aloin B inhibits TPA (HY-18739)-induced ear edema, putrescine elevation, and tumor promotion in mouse skin. Aloin B can be used in research related to anti-inflammation, tumor promotion inhibition, coronavirus disease 2019 (COVID-19) and constipation .
    Aloin B (Standard)
  • HY-183724
    MS8572

    		Deubiquitinase Inflammation/Immunology
    MS8572 is a selective OTUB1 covalent ligand. MS8572 covalently modifies the noncatalytic cysteine 23 residue of OTUB1 and does not inhibit OTUB1 deubiquitinase activity. MS8572 can be used for development of deubiquitinase-targeting chimeras for targeted protein stabilization .
    MS8572
  • HY-135779
    IU2-6

    		Deubiquitinase Neurological Disease
    IU2-6 is a USP14 deubiquitinase inhibitor. IU2-6 inhibits deubiquitinating activity of proteasome-associated USP14, blocks substrate rescue from degradation, and enhances proteasomal activity. IU2-6 can be used for the research of neurodegeneration .
    IU2-6
  • HY-183581
    USP1-IN-18

    		Deubiquitinase DNA/RNA Synthesis Cancer
    USP1-IN-18 is an orally active USP1 inhibitor with a human IC50 of 17.0 nM. USP1-IN-18 inhibits USP1-UAF1 deubiquitinase activity and drives ubiquitinated PCNA accumulation. USP1-IN-18 induces DNA damage, replication stress, and G2-M phase cell cycle arrest. USP1-IN-18 can be used for the research of triple-negative breast cancer .
    USP1-IN-18
  • HY-183604
    T-10531

    		Deubiquitinase Cancer
    T-10531 is a selective USP25/USP28 inhibitor. T-10531 exhibits an IC50 of 0.03 μM and a Kd of 0.2 μM against human USP25, as well as an IC50 of 0.12 μM and a Kd of 0.06 μM against human USP28. T-10531 inhibits USP25/USP28 activity and induces the degradation of USP25 via the proteasomal pathway, without inhibiting other deubiquitinases. T-10531 can be used in the research of squamous cell carcinoma, colorectal cancer, gastric cancer, triple-negative breast cancer and pancreatic cancer .
    T-10531
  • HY-D1236
    Fluorescent brightener 71

    		Parasite Deubiquitinase PARP Cancer
    Fluorescent brightener 71 (FB71) is an inhibitor targeting deubiquitinases UCHL5 and USP14, as well as a CD40 ligand. Fluorescent brightener 71 blocks enzymatic activity, induces apoptosis, inhibits cell growth and triggers reactive oxygen species production. Meanwhile, Fluorescent brightener 71 upregulates the expression of oxidative stress-related genes gpx-4 and sod-4, and reversibly increases the protein levels of UCHL5 and USP14 through a feedback response. Fluorescent brightener 71 inhibits the growth, movement and reproductive capacity of Caenorhabditis elegans, and also exhibits concentration-dependent toxic effects. Fluorescent brightener 71 can be applied to scientific research in related fields such as breast cancer .
    Fluorescent brightener 71
  • HY-182636
    MT16-001

    		Deubiquitinase Aldehyde Dehydrogenase (ALDH) Metabolic Disease Inflammation/Immunology Cancer
    MT16-001 is a cell-permeable UCHL1 inhibitor with an IC50 value of 580 nM. MT16-001 also exhibits considerable inhibitory activity against USP30, and shows selectivity for other UCH family deubiquitinases (DUBs) as well as the broader proteome. MT16-001 binds covalently to the cysteine residue at the active site of UCHL1, and forms covalent interactions with ALDH2, ALDH9A1 and GATD3A in intact cells. Meanwhile, as a cytotoxic agent, it displays a steep dose-response curve in human embryonic kidney cells. MT16-001 can be used for research on various cancers, liver fibrosis and pulmonary fibrosis .
    MT16-001
  • HY-138794G
    XL177A

    		Deubiquitinase SARS-CoV Histone Demethylase Cancer
    XL177A GMP is XL177A (HY-138794) produced by using GMP guidelines. GMP small molecules works appropriately as an auxiliary reagent for cell therapy manufacture. XL177A is a covalent USP7 inhibitor that blocks the deubiquitinase activity of USP7. XL177A destabilizes non-canonical PRC1 complexes or KDM6A and reduces chromatin deposition of H2AK119Ub, thereby relieving the repression of neuronal differentiation programs. Meanwhile, XL177A also regulates the ELOF1-UVSSA-USP7-nuclear β-catenin axis, decreasing the transcription levels of related proteins and the accumulation of nuclear β-catenin. XL177A exerts antiviral effects by reducing the expression levels of coronavirus receptors, and exhibits inhibitory activity against APC-mutated colorectal cancer cells, neuroblastoma, and coronaviruses including SARS-CoV-2 variants. XL177A is mainly used in studies related to colorectal cancer, neuroblastoma, and coronavirus infections .
    XL177A

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