2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. E1/E2/E3 Enzyme

E1/E2/E3 Enzyme

E1 activating enzyme; E2 conjugating enzyme; E3 ligating enzyme; Ubiquitin activating enzyme; Ubiquitin conjugating enzyme; Ubiquitin ligase

E1/E2/E3 Enzyme

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-156767
    Cbl-b-IN-11
    		Inhibitor
    Cbl-b-IN-11 (Compound 466) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 6.4 nM and 6.1 nM, respectively.
    Cbl-b-IN-11
  • HY-163639
    BRD4 degrader-2
    BRD4 degrader-2 (Compound JP-2-197) is a covalent monovalent molecular glue BRD4degrader that induces a ternary complex formation between BRD4 and RNF126. BRD4 degrader-2 targets RNF126 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells.
    BRD4 degrader-2
  • HY-163641
    AR Degrader-1
    AR Degrader-1 (Compound ML 2-9) is a molecular glue androgen receptor (AR) monovalent degrader. AR Degrader-1 degrades AR through DCAF16 (E3 ligase) without obvious cytotoxicity in LNCaP prostate cancer cells.
    AR Degrader-1
  • HY-144099
    Keap1-Nrf2-IN-4
    		Inhibitor
    Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC50=2.55 µM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity.
    Keap1-Nrf2-IN-4
  • HY-N0077R
    Ginkgolic Acid (Standard)
    		Inhibitor
    Ginkgolic Acid (Standard) is the analytical standard of Ginkgolic Acid. This product is intended for research and analytical applications. Ginkgolic Acid is a natural compound that inhibits SUMOylation with an IC50 of 3.0 μM in in vitro assay.
    Ginkgolic Acid (Standard)
  • HY-125660
    Leucettamol A
    		Inhibitor
    Leucettamol A is an inhibitor of Ubc13 (ubiquitin E2 enzyme)-Uev1A interaction, with an IC50 of 50 μg/mL. Leucettamol A can potentially activate the expression of cancer suppressor p53 and is a precursor of anticancer agents. Leucettamol A can be isolated from a marine sponge, Leucetta aff. Microrhaphis.
    Leucettamol A
  • HY-170058
    CRBN ligand-12
    CRBN ligand-12 (Compound 9) is a CRBN-type E3 ubiquitin ligase ligand. CRBN ligand-12 can be used to prepare PROTACs.
    CRBN ligand-12
  • HY-158173
    Cbl-b-IN-19
    		Inhibitor
    Cbl-b-IN-19 (Compound 49) is an inhibitor for casitas B-lineage lymphoma b(Cbl-b), that inhibits Cbl-b phosphorylation with an IC50 < 100 nM.
    Cbl-b-IN-19
  • HY-168601
    WWP1/2-IN-1
    		Inhibitor
    WWP1/2-IN-1 (compound 11) is a WWP1/2 inhibitor with the IC50 values of 32.7µM and 269.2µM for WWP1 and WWP2, respectively.
    WWP1/2-IN-1
  • HY-163518
    Antitumor agent-153
    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.
    Antitumor agent-153
  • HY-168293
    p62-ZZ ligand 1
    p62-ZZ ligand 1 (Compound 7) is an p62-ZZ ligand. p62-ZZ ligand 1 can be used for synthesis of VinclozolinM2-2204 (HY-161741).
    p62-ZZ ligand 1
  • HY-161901
    BC-1293
    		Inhibitor
    BC-1293 is an inhibitor for E3 ligase subunit FBXO24. BC-1293 disrupts the interaction between FBXO24 and aspartyl-tRNA synthetase (DARS2) and increases the level of DARS2. BC-1293 increases levels of IL-1β, IL-9, MIP-2, and TNF α, and exhibits immunostimulatory activity in mice.
    BC-1293
  • HY-175186
    LO-3-62
    LO-3-62 is a PROTAC-like SMARCA2/4 degrader with a truncated fumaramide handle. LO-3-62 degrades SMARCA2/4 in cells.
    LO-3-62
  • HY-170823
    PRC1-IN-1
    		Inhibitor
    PRC1-IN-1 (compound RB-4) is an inhibitor of the polycomb repressive complex PRC1 (IC50=2.3 μM), targeting RING1B-BMI1, RING1A-BMI1, and RING1B-PCGF1 with IC50s of 2.8, 2.6, and 1.8 μM, respectively.
    PRC1-IN-1
  • HY-N0068R
    Solasodine (Standard)
    		Inhibitor
    Solasodine (Standard) is the analytical standard of Solasodine. This product is intended for research and analytical applications. Solasodine (Purapuridine) is a steroidal alkaloid that occurs in plants of the Solanaceae family. Solasodine has neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic and anti-inflammatory activities.
    Solasodine (Standard)
  • HY-128843
    PROTAC MDM2 Degrader-4
    		Inhibitor
    PROTAC MDM2 Degrader-4 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-4 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
    PROTAC MDM2 Degrader-4
  • HY-170515
    RNF5 agonist 1
    		Agonist
    RNF5 agonist 1 (analog-1), a structural analog of RNF5 inhibitor inh-02 (HY-123967), is a potent RNF5 agonist. RNF5 agonist 1 increases the ubiquitylation status of ATG4B in F508del-CFTR-expressing CFBE41o- cells.
    RNF5 agonist 1
  • HY-174416
    Smurf1-IN-5
    		Inhibitor
    Smurf1-IN-5 (Compound cpd-6) is an allosteric SMAD ubiquitin regulatory factor 1 (SMURF1) inhibitor. Smurf1-IN-5 leads to a reduction in the ubiquitylation of substrates such as BMPR2 (bone morphogenetic protein receptor 2) and SMAD1, enhancing the BMP (bone morphogenetic protein) signaling pathway. Smurf1-IN-5 is promising for research of pulmonary arterial hypertension (PAH).
    Smurf1-IN-5
  • HY-142694
    DCN1-UBC12-IN-2
    		Inhibitor
    DCN1-UBC12-IN-2 is a potent and specific DCN1-UBC12 inhibitor (IC50=9.55 nM). DCN1-UBC12-IN-2 could specifically target DCN1-UBC12 interaction and relieve Ang II-induced cardiac fibroblast activation.
    DCN1-UBC12-IN-2
  • HY-156762
    Cbl-b-IN-6
    		Inhibitor
    Cbl-b-IN-6 (Compound 246) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 6.7 nM and 5.2 nM, respectively.
    Cbl-b-IN-6
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity