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 (82):

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-100487
    TAK-243 Inhibitor ≥98.0%
    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-10029
    Nutlin-3a Inhibitor 98.07%
    Nutlin-3a, an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas.
  • HY-12296
    AMG 232 Inhibitor 99.43%
    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-50696
    Nutlin-3 Inhibitor 98.90%
    Nutlin-3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.
  • HY-136339
    Cbl-b-IN-1 Inhibitor 99.00%
    Cbl-b-IN-1 (example 519) is a Cbl-b inhibitor, extracted from patent WO2019148005A1, with an IC50 <100 nM.
  • HY-134656
    BC1618 99.83%
    BC1618, an orally active Fbxo48 inhibitory compound, stimulates Ampk-dependent signaling (via preventing activated pAmpkα from Fbxo48-mediated degradation). BC1618 promotes mitochondrial fission, facilitates autophagy and improves hepatic insulin sensitivity.
  • HY-10949
    SMER3 Inhibitor 98.02%
    SMER3, a Rapamycin enhancer, is a selective Skp1-Cullin-F-box (SCF)Met30 ubiquitin ligase inhibitor. SMER3 enhances Rapamycin's growth inhibitory effect by inhibition of SCFMet30.
  • HY-108702
    ML-792 Inhibitor 99.66%
    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).
  • 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-129395
    CC-92480 Inhibitor 98.02%
    CC-92480, a cereblon E3 ubiquitin ligase modulating drug (CELMoD), acts as a molecular glue. CC-92480 shows high affinity to cereblon, resulting in potent antimyeloma activity.
  • 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-111789
    Subasumstat Inhibitor 98.56%
    Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.
  • HY-120929
    BI8622 Inhibitor 99.35%
    BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM.
  • HY-N0077
    Ginkgolic Acid Inhibitor 98.60%
    Ginkgolic Acid is a natural compound that inhibits SUMOylation with an IC50 of 3.0 μM in in vitro assay.
  • HY-114166
    2-D08 Inhibitor 98.44%
    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-18658
    Siremadlin Inhibitor 99.82%
    Siremadlin (NVP-HDM201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
  • HY-100237
    SZL P1-41 Inhibitor ≥98.0%
    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-100507
    Avadomide Agonist 99.50%
    Avadomide (CC 122) is an orally active cereblon modulator. Avadomide modulates cereblon E3 ligase activity and induces apoptosis of diffuse large B-cell lymphoma (DLBCL) cell lines. Avadomide exhibits potent antitumor and immunomodulatory activities.
  • HY-114312
    MD-224 Inhibitor 99.74%
    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.
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