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 Agonists
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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 Modulators
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E1/E2/E3 Enzyme Inducer
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E1/E2/E3 Enzyme Degraders
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E1/E2/E3 Enzyme Control
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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 (319)
Related Products (319)
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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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NEURL1B-IN-1
0 ImagesCat. No.: HY-182008CAS No.: 3068938-30-4NEURL1B-IN-1 is a molecular glue-like NEURL1B degrader with a Kd value of 46.2 nM. NEURL1B-IN-1 binds to Arg422 within the NHR2 domain of NEURL1B, triggers its autoubiquitination and proteasomal degradation, disrupts its interaction with DLL1, and attenuates the Notch signaling pathway. NEURL1B-IN-1 induces cell cycle arrest and apoptosis, and inhibits migration of hepatocellular carcinoma cells. NEURL1B-IN-1 is applicable to research related to hepatocellular carcinoma.
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PROTAC CCR9 Degrader 1
0 ImagesCat. No.: HY-181287PROTAC CCR9 Degrader 1 is a PROTAC-based degrader targeting CCR9. PROTAC CCR9 Degrader 1 induces ubiquitination, proteasomal degradation of CCR9 and reduces intracellular CCR9 levels by recruiting the VHL E3 ligase. PROTAC CCR9 Degrader 1 has a Ki value of 78.0 nM against human CCR9. PROTAC CCR9 Degrader 1 modulates GPCR activity by binding to the intracellular allosteric binding site of CCR9. PROTAC CCR9 Degrader 1 can be used in research related to Crohn's disease.
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DI-1548
0 ImagesCat. No.: HY-156240CAS No.: 2247060-97-3DI-1548 is a potent, selective, and irreversible covalent inhibitor of DCN1 (IC50 = 4.6 nM). DI-1548 potently and selectively inhibits cullin 3 neddylation at nanomolar concentrations, and exhibits no obvious effect on the neddylation of other cullin members (including cullin 1, 2, 4A, 4B, and 5). DI-1548 exhibits no cytotoxicity. DI-1548 covalently binds to DCN1, disrupting the DCN1-UBC12 interaction, causing the collapse of the neddylation complex, inactivating CRL3, leading to NRF2 accumulation and upregulation of its target genes, and ultimately protecting mice from liver damage. DI-1548 can be used in liver injury research.
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Cbl-b-IN-18
0 ImagesCat. No.: HY-158172CAS No.: 3033320-00-9Cbl-b-IN-18 (compound 51) is an inhibitor of the E3 ligase Casitas B-lineage lymphoma proto-oncogene B (CPL-B). Cbl-b-IN-18 inhibits the phosphorylation of CPL-B (IC50< 100 nM).
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DI-404
0 ImagesCat. No.: HY-122874CAS No.: 2187412-79-7DI-404 is a potent inhibitor of DCN1 with a KKd value of 6.7 nM. DI-404 selectively inhibits neddylation of cullin 3 in a dose-dependent manner.
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5-Octyl-α-ketoglutarate
0 ImagesCat. No.: HY-145452CAS No.: 1616344-00-3Synonyms: 5-Octyl 2-oxopentanedioate5-Octyl-α-ketoglutarate (5-Octyl 2-oxopentanedioate) is a cell-permeable substrate for lysine demethylase. 5-Octyl-α-ketoglutarate is related to protein demethylation, inhibits cell proliferation of wtCRBN expressing cells, and also enhances Lenalidomide (HY-A0003)-induced sensitivity and inhibits myeloma (MM) ) drug resistance of cells. When myeloma (MM) cells undergo glutamine-dependent proliferation, α-ketoglutarate increases glutamine catabolism to promote protein demethylation.
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Panepophenanthrin
0 ImagesCat. No.: HY-169796CAS No.: 409064-57-9Panepophenanthrin is a compound that can be isolated from the mushroom strain, Panus rudis Fr. IFO 8994. Panepophenanthrin is a ubiquitin-activating enzyme inhibitor.
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Solasodine hydrochloride
0 ImagesCat. No.: HY-W751400CAS No.: 6106-33-8Synonyms: Purapuridine hydrochloride; Solancarpidine hydrochloride; Solasodin hydrochlorideSolasodine (Purapuridine) hydrochloride is a steroidal alkaloid that occurs in plants of the Solanaceae family. Solasodine hydrochloride induces apoptosis by inhibiting the p53-MDM2 complex, p21Waf1/Cip1, and Bcl-2 proteins. Solasodine hydrochloride has neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic and anti-inflammatory activities.
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Milademetan tosylate hydrate (Standard)
0 ImagesCat. No.: HY-101266BRCAS No.: 2095625-97-9Synonyms: DS-3032b (Standard); DS-3032 tosylate hydrate (Standard)Milademetan (tosylate hydrate) (Standard) is the analytical standard of Milademetan (tosylate hydrate) (HY-101266B). This product is intended for research and analytical applications. Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis.
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Heclin (Standard)
0 ImagesCat. No.: HY-110204RCAS No.: 890605-54-6Heclin (Standard) is the analytical standard of Heclin (HY-110204). This product is intended for research and analytical applications. Heclin is a HECT E3 ubiquitin ligases inhibitor. Heclin inhibits Smurf2, Nedd4, WWP1 (IC50 values are 6.8, 6.3, 6.9 μM) and can be used for the research of gastric cancer.
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Americanin A
0 ImagesCat. No.: HY-N18301CAS No.: 69506-79-2Americanin A is a Neolignan. Americanin A can be isolated from the seeds of Phytolacca americana. Americanin A activates ATM and ATR, initiating the subsequent signal transduction cascades that include Chk1, Chk2, and tumor suppressor p53. Americanin A targets selectively Skp2 for degradation and thereby stabilizes p27. Americanin A suppresses the activity of Cyclin B1 and its partner cdc2 to prevent entry into Mitosis. Americanin A induces Apoptosis by producing excessive ROS. Americanin A has anti-cancer activity against colorectal cancer.
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Milademetan (Standard)
0 ImagesSynonyms: DS-3032 (Standard)Milademetan (Standard) is the analytical standard of Milademetan (HY-101266). This product is intended for research and analytical applications. Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.
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NRX-252262 (Standard)
0 ImagesCat. No.: HY-111760RCAS No.: 2438637-61-5NRX-252262 (Standard) is the analytical standard of NRX-252262 (HY-111760). This product is intended for research and analytical applications. NRX-252262 is a potent enhancer of the interaction between β-Catenin, and its cognate E3 ligase, SCFβ-TrCP, induces mutant β-catenin degradation, with an EC50 of 3.8 nM.
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TAK-243 (Standard)
0 ImagesCat. No.: HY-100487RCAS No.: 1450833-55-2Synonyms: MLN7243 (Standard)TAK-243 (Standard) is the analytical standard of TAK-243 (HY-100487). This product is intended for research and analytical applications. TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
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MRT-31619 formate
0 ImagesCat. No.: HY-180538APurity: 99.28%MRT-31619 formate is a molecular gel degrader (MGD) targeting CRBN. MRT-31619 formate drives the self-dimerization of the E3 ligase by mimicking the degradation subunit, and promotes its rapid, effective and selective degradation through the ubiquitin-proteasome system.
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GS143 (Standard)
0 ImagesCat. No.: HY-110261RCAS No.: 916232-21-8GS143 (Standard) is the analytical standard of GS143 (HY-110261). This product is intended for research and analytical applications. GS143 is a selec-tive IκBα ubiquitination inhibitor with an IC50 of 5.2 μM for SCFβTrCP1-mediated IκBα ubiquitylation. GS143 sup-presses NF-κB acti-va-tion and tran-scrip-tion of tar-get genes and does not inhibit proteasome activity. GS143 has anti-asthma effect.
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Avadomide (Standard)
0 ImagesSynonyms: CC 122 (Standard)Avadomide (Standard) is the analytical standard of Avadomide. This product is intended for research and analytical applications. Avadomide is an orally active cereblon modulator. Avadomide 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 exhibits potent antitumor and immunomodulatory activities.
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ML-792 (Standard)
0 ImagesCat. No.: HY-108702RCAS No.: 1644342-14-2ML-792 (Standard) is the analytical standard of ML-792 (HY-108702). This product is intended for research and analytical applications. ML-792 is a potent and selective inhibitor of SAE/SUMO1 and SAE/SUMO2 in enzymatic assays (IC50 values of 3 and 11 nM, respectively) compared with NAE/NEDD8 and UAE/ubiquitin (IC50> values of 32 μM and >100 μM, respectively).
