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

E1/E2/E3 Enzyme

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.

E1/E2/E3 Enzyme Related Products (62):

Cat. No. Product Name Effect Purity
  • HY-15676
    Idasanutlin Inhibitor 99.90%
    Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM.
  • HY-12296
    AMG 232 Inhibitor 99.90%
    AMG 232 is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. AMG 232 binds to MDM2 with a Kd of 0.045 nM.
  • HY-10029
    Nutlin (3a) Inhibitor 98.07%
    Nutlin 3a is an active enantiomer of Nutlin-3, acts as a murine double minute (MDM2) inhibitor that inhibits MDM2-p53 interactions and stabilizes the p53 protein, and thereby induces cell cycle arrest and apoptosis.
  • HY-50696
    Nutlin (3) Inhibitor 98.32%
    Nutlin 3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.
  • HY-100487
    TAK-243 Inhibitor 99.43%
    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.
  • HY-114312
    MD-224 Inhibitor
    MD-224 is a first-in-class and highly potent small-molecule human murine double minute 2 (MDM2) degrader based on the proteolysistargeting chimera (PROTAC) concept. MD-224 induces rapid degradation of MDM2 at concentrations <1 nM in human leukemia cells, and achieves an IC50 value of 1.5 nM in inhibition of growth of RS4;11 cells. MD-224 has the potential to be a new class of anticancer agent.
  • HY-128842
    PROTAC MDM2 Degrader-3 Inhibitor
    PROTAC MDM2 Degrader-3 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-3 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
  • HY-125858
    MI-1061 Inhibitor 98.22%
    MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53, induces apoptosis, and has anti-tumor activity.
  • HY-10959
    RG7112 Inhibitor 99.91%
    RG7112 is a potent, selective, first clinical, orally active and blood-brain barrier crossed MDM2-p53 inhibitor, with an IC50 of 18 nM and a KD of 11 nM for binding to MDM2.
  • HY-N0077
    Ginkgolic Acid Inhibitor 99.59%
    Ginkgolic Acid is a natural compound that inhibits SUMOylation with an IC50 of 3.0 μM in in vitro assay.
  • HY-13296
    PYR-41 Inhibitor >98.0%
    PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
  • HY-100507
    Avadomide Agonist 99.53%
    Avadomide (CC 122) is an orally available cereblon modulator. Avadomide modulates cereblon E3 ligase activity and exhibits potent antitumor and immunomodulatory activities.
  • HY-18658
    Siremadlin Inhibitor 99.19%
    Siremadlin (NVP-HDM201) is a potent and highly specific MDM-2/p53 inhibitor.
  • HY-103236
    NSC232003 Inhibitor 98.09%
    NSC232003 is a highly potent and cell-permeable UHRF1 inhibitor, which inhibits DNA methylation in vitro and disrupts DNMT1/UHRF1 interactions at a cellular level.
  • HY-100237
    SZL P1-41 Inhibitor 99.18%
    SZL P1-41 is a specific Skp2 inhibitor, binds to the F-box domain of Skp2 to prevent Skp1 association and Skp2 SCF complex formation. SZL P1-41, like Skp2 deficiency, augments p27-mediated apoptosis/senescence, while it impairs Akt-driven glycolysis. Anti-tumor activities.
  • HY-114166
    2-D08 Inhibitor 99.04%
    2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 also inhibits Axl with an IC50 of 0.49 nM.
  • HY-17493
    MI-773 Inhibitor >98.0%
    MI-773 is a new small molecule inhibitor of the MDM2-p53 interaction, binds to MDM2 with high affinity (Ki=0.88 nM) and blocks the p53-MDM2 interaction.
  • HY-18986
    SAR405838 Inhibitor
    SAR405838 is a highly potent and selective MDM2 inhibitor, binds to MDM2 with Ki= 0.88 nM and has high specificity over other proteins.
  • HY-108702
    ML-792 Inhibitor 99.66%
    ML-792 is a specific small ubiquitin-like modifier (SUMO)-activating enzyme (SAE) inhibitor. ML-792 is a potent and selective inhibitor of SAE/SUMO1 and SAE/SUMO2 in enzymatic assays (IC50s of 3 and 11 nM, respectively) compared with NAE/NEDD8 and UAE/ubiquitin (IC50s of 32 μM and >100 μM, respectively).
  • HY-120929
    BI8622 Inhibitor 99.35%
    BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM.
Isoform Specific Products

Your Search Returned No Results.

Sorry. There is currently no product that acts on isoform together.

Please try each isoform separately.