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deubiquitinase

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Cat. No. Nombre del producto Target Áreas de investigación 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-141659
    CMPD-39
    3 Publications Verification

    Mitophagy Deubiquitinase Neurological Disease
    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 .
    CMPD-39
  • 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

    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

    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-143345

    Deubiquitinase Cancer
    EN523 is a OTUB1 recruiter. EN523 targets a non-catalytic allosteric cysteine C23 in the K48-ubiquitin-specific deubiquitinase OTUB1 .
    EN523
  • HY-141852

    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-153627

    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-143344

    PROTACs CFTR Inflammation/Immunology
    NJH-2-056 is a deubiquitinase-targeting chimera (DUBTAC) linking the OTUB1 recruiter EN523 to the CFTR chaperone lumacaftor. NJH-2-056 can be used for cystic fibrosis research .
    NJH-2-056
  • HY-148482

    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-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-D2188

    Deubiquitinase Cancer
    IMP-2373 is a low-toxicity activity-based probe targeting covalent pan-deubiquitinase (DUB), which modulates and monitors DUB activity via covalent binding to the catalytic cysteine and active site of DUB. IMP-2373 enables real-time tracking of dynamic intracellular DUB activity in physiologically relevant living cell systems, and quantitative analysis of activity changes induced by pharmacological inhibition or MYC dysregulation. IMP-2373 can be used for research on related diseases such as B-cell lymphoma .
    IMP-2373
  • 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-138978

    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-149902

    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-114383

    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-149901

    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-144999

    Wee1 Cancer
    LEB-03-146 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through a PEG2 linker. LEB-03-146 shows significant WEE1 stabilization in HEP3B hepatoma cancer cells .
    LEB-03-146
  • HY-148481

    Deubiquitinase Cancer
    USP7-IN-10 (compound 1) is a potent ubiquitin-specific protease 7 (USP7) inhibitor, with an IC50 of 13.39 nM .
    USP7-IN-10
  • HY-D1726

    Deubiquitinase Cancer
    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-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-172193

    SGC-UBD1031

    Deubiquitinase HDAC Inflammation/Immunology Cancer
    UBD1031 (SGC-UBD1031) is a selective USP16/HDAC6-UBD antagonist with a human USP16-UBD IC50 of 10.6 μM, KD value of 48 nM, and a human HDAC6-UBD KD of 16 nM. UBD1031 disrupts ISG15 C-terminus interactions with USP16-UBD and HDAC6-UBD, and exhibits cooperative inhibition of full-length USP16 deubiquitinase activity via USP16-UBD binding. UBD1031 can be used in research on cancer, autoimmune diseases, and Down syndrome .
    UBD1031
  • HY-143342

    Wee1 Cancer
    LEB-03-144 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through a C3 alkyl linker. LEB-03-144 shows significant WEE1 stabilization in HEP3B hepatoma cancer cells .
    LEB-03-144
  • HY-162966

    Cyclic GMP-AMP Synthase PROTACs STING Cancer
    MS7829 is a deubiquitinase-targeting chimera (DUBTAC) that targets cGAS. MS7829 recruits OTUB1 to cGAS, binds covalently to OTUB1, stabilizes the protein abundance of cGAS, and activates the cGAS-STING-IRF3 innate immune signaling pathway in an OTUB1-dependent manner. MS7829 is applicable to cancer-related research .
    MS7829
  • HY-138794A

    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-158774

    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-176416

    Deubiquitinase Cancer
    USP7-IN-17 (compound M15) is a potent USP7 inhibitor. USP7-IN-17 inhibits HepG2 cell activity with an IC50 of 4.38 μM .
    USP7-IN-17
  • HY-172220

    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-174301

    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

    Deubiquitinase Cancer
    FX-171-C is a noncompetitive Deubiquitinase inhibitor with an IC50 of 1.4 µM .
    FX-171-C
  • HY-162967

    PROTACs Cyclic GMP-AMP Synthase STING Inflammation/Immunology Cancer
    MS8588 is a deubiquitinase-targeting chimera (DUBTAC) against cGAS. MS8588 induces targeted stabilization of cGAS, thereby activating downstream signaling pathways. MS8588 activates the cGAS/STING/IRF3 innate immune signaling pathway. MS8588 exhibits antitumor activity .
    MS8588
  • HY-143343

    Wee1 Cancer
    LEB-03-153 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through no linker .
    LEB-03-153
  • HY-169154

    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

    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-143340

    Wee1 Cancer
    LEB-03-145 is a WEE1 DUBTAC (deubiquitinase-targeting chimera) linking AZD1775 (Adavosertib) to the OTUB1 recruiter EN523 through a C5 alkyl linker .
    LEB-03-145
  • HY-163769

    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

    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

    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

    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-182350

    DUBTACs Deubiquitinase Metabolic Disease
    FXR DUBTAC modulator-1 is a deubiquitinase-targeting chimeric molecule (DUBTAC) that targets FXR, with a Ka value of 2.12e-5 M for FXR. FXR DUBTAC modulator-1 recruits the deubiquitinase OTUB1, binds to OTUB1 and forms a ternary complex with FXR, reduces the polyubiquitination level of FXR, prevents FXR degradation via the ubiquitin-proteasome pathway, and elevates the protein level of FXR. FXR DUBTAC modulator-1 can be used in the research of cholestatic liver injury .
    FXR DUBTAC modulator-1
  • HY-185122

    CFTR Deubiquitinase Cancer
    MS6178 is a MS5105-based CFTR deubiquitinase-targeted chimera (DUBTAC) that recruits OTUB1 to stabilize ΔF508-CFTR mutant protein in a concentration- and time-dependent manner, with an OTUB1-dependent effect and no impact on CFTR mRNA level. MS6178 can be used for the research of cancer .
    MS6178
  • HY-183725

    DUBTACs Deubiquitinase CFTR Inflammation/Immunology
    MS5128 is an OTUB1-based deubiquitinase-targeting chimera (DUBTAC) targeting CFTR. MS5128 recruits OTUB1 to CFTR to induce deubiquitination and stabilization of CFTR. MS5128 can be used for the research of cystic fibrosis . (Blue: CFTR Ligand (HY-183724); Pink: OTUB1 Ligand (HY-13262); Black: Linker)
    MS5128
  • HY-183581

    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

    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-182636

    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

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