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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
25 Results for "
deubiquitinase activity
" in MedChemExpress (MCE) Product Catalog:
Products (25)
25 Results for "deubiquitinase activity" in MCE Product Catalog:
26
26 Publications Verification
Target:
Research Areas:
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 .
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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.
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6 Cited Publications
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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 .
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Category:
Quinones Liliaceae Anthraquinones Other Diseases Aloe vera (L.) Burm. f. Phenols Polyphenols Plants Disease Research Fields
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1 Cited Publications
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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 .
Cat. No.: HY-176426
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Research Areas:
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 .
Cat. No.: HY-145337
Purity: 99.93%
Synonyms: FT385
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Research Areas:
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 .
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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 .
Cat. No.: HY-D2188
Cat. No.: HY-172193
Synonyms: SGC-UBD1031
Target:
Research Areas:
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 .
Cat. No.: HY-138794A
CAS No.: 2417089-73-5
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(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 .
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 .
Cat. No.: HY-174301
CAS No.: 3052223-40-9
Research Areas:
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.
Cat. No.: HY-164689
CAS No.: 18897-36-4
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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 .
Cat. No.: HY-163769
CAS No.: 3052553-77-9
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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 .
Cat. No.: HY-162967
CAS No.: 3060519-94-7
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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 .
Cat. No.: HY-N0886R
CAS No.: 28371-16-6
Synonyms: Isobarbaloin (Standard)
Cat. No.: HY-135779
CAS No.: 1356074-25-3
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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 .
Cat. No.: HY-183724
CAS No.: 3060517-63-4
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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 .
Cat. No.: HY-187197
CAS No.: 3132184-09-6
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GL-637 is a covalent and selective inhibitor of SARS-CoV-1/2 papain-like protease (PLpro), with IC50 values of 42.4 nM and 50.5 nM against the two viruses, respectively. GL-637 covalently modifies the catalytic Cys111 of PLpro, binds to Glu167 and occupies the BL2 groove, thereby inhibiting the deubiquitinase and deISGylase activities of PLpro. GL-637 can be used in the research of coronaviruses .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
