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 (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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PROTAC SKP2 Degrader-1
0 ImagesPROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a Kd value of 6.28 μM. PROTAC SKP2 Degrader-1 induces targeted degradation of SKP2 via the ubiquitin-proteasome system. PROTAC SKP2 Degrader-1 stabilizes the expression of SOCS1 and regulates the expression of immunoproteasomes through the JAK/STAT pathway, thereby inhibiting tumor cell proliferation. PROTAC SKP2 Degrader-1 is applicable for cancer-related research.
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JWZ-8-103 hydrochloride
0 ImagesCat. No.: HY-180654APurity: 99.93%JWZ-8-103 hydrochloride is an orally active analog of PRLX-93936 (HY-119264) and a molecular glue targeting TRIM21. JWZ-8-103 hydrochloride increases the thermal stability of TRIM21. JWZ-8-103 hydrochloride promotes rapid and efficient interaction between TRIM21 and NUP98 (the apparent EC50 for ternary complex formation with the PRYSPRY domain of TRIM21 and the APD domain of NUP98 is approximately 20 μM), induces extensive ubiquitination and proteasomal degradation of numerous adjacent nucleoporins (NUPs, and thereby triggers cellular apoptosis. JWZ-8-103 hydrochloride can be used for the research of pancreatic cancer.
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Cbl-b-IN-9
0 ImagesCbl-b-IN-9 (Compound 300) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 5.6 nM and 4.7 nM, respectively.
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DDO-4033
0 ImagesCat. No.: HY-175247Purity: 99.11%DDO-4033 is a SPOP inhibitor (IC50 = 16.9 μM, Kd = 15.1 μM). DDO-4033 impairs the malignant migration, invasion, and proliferation of clear cell renal cell carcinoma (ccRCC) cell lines. DDO-4033 disrupts SPOP recruitment to its substrate LATS1, inhibits its polyubiquitination and subsequent degradation, and upregulates LATS1 expression. DDO-4033 has promising antitumor activity and is promising for renal cell carcinoma research.
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RNF5-IN-1
0 ImagesRNF5-IN-1 is a selective small-molecule inhibitor and degrader of the E3 ubiquitin ligase RNF5. RNF5-IN-1 directly binds to the N-terminal cytosolic domain of RNF5 with a KD of 594 nM, inhibits the E3 ubiquitin ligase activity of RNF5, and exhibits selectivity over Hrd1 and Praja1. RNF5-IN-1 promotes the degradation of RNF5 via the p97/VCP-dependent endoplasmic reticulum-associated degradation (ERAD) and proteasome pathway. RNF5-IN-1 inhibits the retrotranslocation of misfolded proteins. RNF5-IN-1 is applicable for research on mechanisms related to cystic fibrosis.
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Teslexivir hydrochloride
0 ImagesSynonyms: BTA074 hydrochloride; AP 611074 hydrochlorideTeslexivir (BTA074) hydrochloride is a potent antiviral agent. Teslexivir hydrochloride 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 hydrochloride can be used for condyloma research.
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TRAF6 peptide TFA
0 ImagesCat. No.: HY-P3709APurity: 98.20%TRAF6 peptide TFA is a specific TRAF6-p62 inhibitor. TRAF6 peptide TFA potently abrogates NGF-dependent TrkA ubiquitination. TRAF6 peptide TFA has good research potential in neurological diseases such as alzheimer's disease (AD), parkinson's, ALS, head trauma, epilepsy and stroke.
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Antitumor agent-153
0 ImagesCat. No.: HY-163518Purity: 99.62%Antitumor agent-153 (compound 11b) is an optimized H2A histone ubiquitination inhibitor based on PRT4165 (HY-19817). Antitumor agent-153 inhibits the viability of human osteosarcoma U2OS cells and reduces histone H2A monoubiquitination, exhibiting anticancer activity.
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MRC37
0 ImagesCat. No.: HY-180548Purity: 98.90%MRC37 is a high-affinity TRIM21 ligand with a Kd of 0.4 µM. MRC37 targets the IgG Fc-binding pocket in the PRYSPRY domain of TRIM21, mimics the "HHNY" epitope, and inhibits substrate-induced aggregation and activation of TRIM21 via competitive blockade of antibody binding. MRC37 effectively blocks TRIM21-mediated antiviral immunity (such as adenovirus neutralization) and Trim-Away targeted protein degradation without cytotoxicity. MRC37 antagonizes TRIMTAC activity, and its multiple modification sites do not affect target binding, making it suitable as a degrader warhead for research on viral immunity and neurodegenerative diseases such as tauopathies.
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dGEM3
0 ImagesCat. No.: HY-173366Purity: 99.22%dGEM3 is a selective GEMIN3 Molecular glue degrader with a DC50 of 680 nM. dGEM3 recruits GEMIN3 to the VHL E3 ligase, and mediates the targeted ubiquitination and degradation of GEMIN3 via the ubiquitin-proteasome system. dGEM3 induces extensive transcriptomic changes, including upregulation of ER stress response genes and downregulation of mRNA splicing genes. dGEM3 can be used in research related to amyotrophic lateral sclerosis, spinal muscular atrophy and neuromuscular dysfunction.
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p53-MDM2-IN-1
0 Imagesp53-MDM2-IN-1 (Example 30) is an inhibitor of p53-MDM2/X protein interaction with an Ki value of 23.35 µM. p53-MDM2-IN-1 can be used for anti-tumor research.
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Cbl-b-IN-13
0 ImagesCbl-b-IN-13 (Example 520) is a Cbl-b inhibitor with an IC50 of <100 nM. Cbl-b-IN-13 has the ability to activate T-cells.
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Indole-3-carbinol (Standard)
0 ImagesIndole-3-carbinol (Standard) is the analytical standard of Indole-3-carbinol. This product is intended for research and analytical applications. Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).
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BMS-986482
0 ImagesCat. No.: HY-182467CAS No.: 3062993-48-7BMS-986482 is a CRBN-mediated IKZF1-4 (Ikaros family zinc finger 1-4) molecular glue degrader. BMS-986482's activity is driven by a non-traditional CELMoD core that selectively degrades the IKZF protein family. BMS-986482 can be used for the research of advanced solid tumors.
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PROTAC RNF4 degrader-1
0 ImagesCat. No.: HY-181692Purity: 98.09%PROTAC RNF4 degrader-1 is a RNF4 PROTAC degrader (Kd = 64.5 nM) that degrades RNF4 via the ubiquitin-proteasome system. PROTAC RNF4 degrader-1 induces DNA damage, apoptosis, and exhibits antiproliferative activity in cancer cells. PROTAC RNF4 degrader-1 displays antitumor activity with no obvious side effects in mouse models. PROTAC RNF4 degrader-1 is applicable to the research of hepatocellular carcinoma.
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Cbl-b-IN-2
0 ImagesCat. No.: HY-141431CAS No.: 2503325-21-9Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent.
