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-157728
    ML307
    		Inhibitor 99.10%
    ML307 is a potent, sub-micromolar, first-in-class Ubc13 enzyme activity inhibitor with an IC50 of 781 nM. ML307 has the potential for immunomodulation and inflammation research.
    ML307
  • HY-134597
    SENP1-IN-4
    		Inhibitor ≥98.0%
    SENP1-IN-4 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 21. SENP1-IN-4 is developed for tumor radiosensitivity enhancement.
    SENP1-IN-4
  • HY-P3709
    TRAF6 peptide
    		Inhibitor
    TRAF6 peptide is a specific TRAF6-p62 inhibitor. TRAF6 peptide potently abrogates NGF-dependent TrkA ubiquitination. TRAF6 peptide has good research potential in neurological diseases such as alzheimer's disease (AD), parkinson's, ALS, head trauma, epilepsy and stroke.
    TRAF6 peptide
  • HY-109045
    Teslexivir
    		Inhibitor
    Teslexivir (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.
    Teslexivir
  • HY-70027
    p53 and MDM2 proteins-interaction-inhibitor (chiral)
    		Inhibitor 98.13%
    p53 and MDM2 proteins-interaction-inhibitor (chiral) (Compound 32) is an inhibitor of the interaction between p53 and MDM2 proteins.
    p53 and MDM2 proteins-interaction-inhibitor (chiral)
  • HY-126075
    WS-383 free base
    		Inhibitor
    WS-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.
    WS-383 free base
  • HY-100507A
    Avadomide hydrochloride
    		Modulator
    Avadomide 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.
    Avadomide hydrochloride
  • HY-169005
    Cbl-b-IN-27
    		Inhibitor
    Cbl-b-IN-27 is a casitas B-lymphoma proto-oncogene-b (Cbl-b) inhibitor with an IC50 value of 7 nM. Cbl-b-IN-27 is promising for research of effector T cell function, T cell, natural killer (NK) cell and B cell activation regulation.
    Cbl-b-IN-27
  • HY-D2259
    PFI-7
    PFI-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.
    PFI-7
  • HY-100765
    BI-0252
    		Inhibitor
    BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis.
    BI-0252
  • HY-156763
    Cbl-b-IN-7
    		Inhibitor
    Cbl-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.
    Cbl-b-IN-7
  • HY-134595
    SENP1-IN-2
    		Inhibitor
    SENP1-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.
    SENP1-IN-2
  • HY-131667
    Hdm2 E3 ligase inhibitor 1
    		Inhibitor
    Hdm2 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.
    Hdm2 E3 ligase inhibitor 1
  • HY-156373
    MN714
    		Inhibitor
    MN714 is a pivaloyloxymethyl (POM) protected inhibitor.
    MN714
  • HY-158171
    Cbl-b-IN-17
    		Inhibitor
    Cbl-b-IN-17 (Example-40) is an inhibitor of Cbl-b with an IC50 value <100 nM.
    Cbl-b-IN-17
  • HY-12296S
    Navtemadlin-d7
    		Inhibitor
    Navtemadlin-d7 is the deuterium labeled Navtemadlin. Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM.
    Navtemadlin-d<sub>7</sub>
  • HY-163809
    BRD9 Degrader-2
    BRD9 Degrader-2 (Compound B11) is a BRD9 degrader (DC50 ≤1.25 nM; Dmax≥75%). BRD9 Degrader-2 can be used for research of cancers.
    BRD9 Degrader-2
  • HY-168243
    E3 ligase Ligand 36
    E3 ligase Ligand 36 is an E3 ligase Ligand, and can be used for synthesis of PROTACs, such as PROTAC BRM/BRG1 degrader-1 (HY-168242).
    E3 ligase Ligand 36
  • HY-156764
    Cbl-b-IN-8
    		Inhibitor
    Cbl-b-IN-8 (Compound 293) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 5.5 nM and 7.8 nM, respectively.
    Cbl-b-IN-8
  • HY-155477
    Cbl-b-IN-15
    		Inhibitor
    Cbl-b-IN-15 (compound 25) is an inhibitor of the RING finger E3 ligase Cbl (IC50: 15 nM). Cbl-b refers to Casitas B-lineage lymphoma proto-oncogene-b, which inhibits T-cell, natural killer (NK) cell, and B-cell activation. Cbl-b-IN-15 activates T cell function with EC50=0.41 μM.
    Cbl-b-IN-15
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity