E1/E2/E3 Enzyme
E1 activating enzyme; E2 conjugating enzyme; E3 ligating enzyme; Ubiquitin activating enzyme; Ubiquitin conjugating enzyme; Ubiquitin ligase
Ubiquitin (UB) is a protein modifier that regulates many essential cellular processes. To initiate protein modification by UB, the E1 enzyme activates the C-terminal carboxylate of UB to launch its transfer through the E1-E2-E3 cascade onto target proteins. The E1 enzyme is the activating enzyme, to which ubiquitin is attached in an ATP-dependent reaction by a thioester bond. The E2 enzyme is the conjugating enzyme, to which the ubiquitin is transferred from the E1. The E3 is the ubiquitin ligase, which directly or indirectly catalyzes the transfer of the ubiquitin to the target protein (the substrate), with the formation of an isopeptide bond.
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E1/E2/E3 Enzyme Inhibitors
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E1/E2/E3 Enzyme Antagonist
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E1/E2/E3 Enzyme Activators
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E1/E2/E3 Enzyme Degraders
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E1/E2/E3 Enzyme Ligands
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Ubiquitin Enzymes Proteins
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E1/E2/E3 Enzyme Related Products (320)
Related Products (320)
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Recombinant Proteins (116)
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Antibodies (88)
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Related Compound Screening Libraries (1)
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Teslexivir
0 ImagesCat. No.: HY-109045CAS No.: 1075798-37-6Synonyms: BTA074; AP 611074Teslexivir (BTA074) is a potent antiviral agent. Teslexivir is a potent and selective inhibitor of the interaction between two essential viral proteins, E1 and E2, an association that is a necessary step in the DNA replication and thus viral production for Human Papilloma Virus (HPV) 6 and 11. Teslexivir can be used for condyloma research.
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YH239-EE
0 ImagesYH239-EE, ethyl ester of the free carboxylic acid compound YH239, is a potent p53-MDM2 antagonizing and apoptosis-inducing agent.
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(Rac)-Nutlin-3
0 ImagesSynonyms: (Rac)-Rebemadlin(Rac)-Nutlin-3 (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). (Rac)-Nutlin-3 inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. (Rac)-Nutlin-3 has the potential for the study of TP53 wild-type ovarian carcinomas.
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WS-383 free base
0 ImagesCat. No.: HY-126075CAS No.: 2247543-65-1WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
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XYD113
0 ImagesCat. No.: HY-184896CAS No.: 3032314-99-8XYD113 is an orally active, selective GSPT1 Molecular glue degrader. XYD113 promotes the formation of the CRBN-GSPT1 ternary complex and mediates GSPT1 degradation in a CRBN-dependent manner via the ubiquitin-proteasome system. XYD113 downregulates genes associated with the occurrence and progression of prostate cancer (c-Myc, AR, AR-V7, KLK3, KLK2, TMPRSS2). XYD113 exhibits anticancer activity against prostate cancer. XYD113 can be used in the research of prostate cancer.
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Avadomide hydrochloride
0 ImagesCat. No.: HY-100507ACAS No.: 1398053-45-6Synonyms: CC 122 hydrochlorideAvadomide hydrochloride (CC 122 hydrochloride) is the hydrochloride form of Avadomide (HY-100507). Avadomide hydrochloride is an orally active cereblon modulator. Avadomide hydrochloride modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide hydrochloride exhibits potent antitumor and immunomodulatory activities.
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PFI-7
0 ImagesCat. No.: HY-D2259CAS No.: 2910938-58-6PFI-7 is a probe, which binds to human GID4 (KD is 79 nM), and antagonizes the binding of Pro/N-degrons. PFI-7 can be utilized in C-terminal to LisH (CTLH) complex research and development of targeted protein degradation.
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UBA5-IN-2
0 ImagesCat. No.: HY-178458UBA5-IN-2 (Compound 50) is a potent ubiquitin-like modifier activating enzyme 5 (UBA5) inhibitor (IC50=0.063 μM). UBA5-IN-2 is promising for research of cancers and protein homeostasis-related diseases.
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BI-0252
0 ImagesCat. No.: HY-100765CAS No.: 1818291-27-8
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JWP24 acetate
0 ImagesCat. No.: HY-P11621APurity: 98.48%JWP24 acetate is the first cell membrane-permeable peptide inhibitor of MAGE-A4, with an IC50 of 200 nM against human MAGE-A4. JWP24 acetate binds to intracellular targets while retaining binding activity, disrupts the interaction between MAGE-A4 and RAD18, and does not induce cytotoxicity at effective concentrations. JWP24 acetate is applicable for cancer-related research.
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dTAG-TRIMTAC
0 ImagesCat. No.: HY-185652CAS No.: 3070832-72-0dTAG-TRIMTAC is a PROTAC-like degrader targeting TRIM21. dTAG-TRIMTAC forms a ternary complex with TRIM21 and target proteins to drive degradation of oligomeric/assembled substrates via TRIM21 clustering-based activation, with degradation dependent on endogenous TRIM21. dTAG-TRIMTAC can be used for the research of neurodegenerative disease and inflammatory disease.
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Thalidomide-C1-O-CO-C2-Piperazine-CO-C1-Azacyclohexane-C1-Piperazine
0 ImagesCat. No.: HY-178518Thalidomide-C1-O-CO-C2-Piperazine-CO-C1-Azacyclohexane-C1-Piperazine is an E3 ligase ligand-linker conjugate containing a cereblon (CRBN) ligand for E3 ubiquitin ligase and a linker. Thalidomide-C1-O-CO-C2-Piperazine-CO-C1-Azacyclohexane-C1-Piperazine can be used to synthesize PROTAC CDK4/6/9 degrader 2 (HY-178516).
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JWP24
0 ImagesCat. No.: HY-P11621JWP24 is the first cell membrane-permeable peptide inhibitor of MAGE-A4, with an IC50 of 200 nM against human MAGE-A4. JWP24 binds to intracellular targets while retaining binding activity, disrupts the interaction between MAGE-A4 and RAD18, and does not induce cytotoxicity at effective concentrations. JWP24 is applicable for cancer-related research.
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Cbl-b-IN-7
0 ImagesCat. No.: HY-156763CAS No.: 2815221-35-1Cbl-b-IN-7 (Compound 248) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 6.7 nM and 5.2 nM, respectively.
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SENP1-IN-2
0 ImagesCat. No.: HY-134595CAS No.: 2416910-70-6SENP1-IN-2 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 30. SENP1-IN-2 is developed for tumor radiosensitivity enhancement.
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Cbl-b-IN-33
0 ImagesCat. No.: HY-183997CAS No.: 2815221-18-0Cbl-b-IN-33 is an orally active, selective inhibitor of Casitas B-lineage lymphoma-b (Cbl-b) with an IC50 of 7 nM and a Kd of 1.2 nM. Cbl-b-IN-33 inhibits non-phosphorylated E3 ubiquitin ligase Cbl-b, induces IL-2 activation in peripheral blood mononuclear cells, and exerts tumor growth inhibitory effects in a mouse colon cancer model. Cbl-b-IN-33 can be used for the research of colon cancer.
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T7117
0 ImagesCat. No.: HY-183638CAS No.: 162060-03-9T7117 is a TRIM25-HIF-1α inhibitor. T7117 disrupts the interaction between TRIM25-HIF-1α. T7117 can be used for the research of glioblastoma.
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Obudanersen sodium scrambled negative control
0 ImagesCat. No.: HY-177651BObudanersen sodium scrambled negative control is the sequence scrambled negative control of Obudanersen sodium.
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Hdm2 E3 ligase inhibitor 1
0 ImagesCat. No.: HY-131667CAS No.: 414905-09-2Hdm2 E3 ligase inhibitor 1 (Compound 1) is a reversible inhibitor for Hdm2 (an E3 ubiquitin ligase)-mediated ubiquitination of the p53 protein with an IC50 of 12.7 μM. Hdm2 E3 ligase inhibitor 1 binds Hdm2, blocks Hdm2-catalyzed ubiquitin transfer from preligated Ub-Ubc4 to p53, inhibits p53 ubiquitination, stabilizes p53 protein in tumor cell and exhibits antitumor efficacy.
