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-128841
    PROTAC MDM2 Degrader-2
    		Inhibitor
    PROTAC MDM2 Degrader-2 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-2 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase (CN108610333A).
    PROTAC MDM2 Degrader-2
  • HY-148602
    KH-4-43
    		Inhibitor 99.99%
    KH-4-43 is an inhibitor of E3 CRL4. KH-4-43 inhibits E3 CRL4's core ligase complex and exhibits anticancer activity. KH-4-43 has a binding Kd to E3 ROC1-CUL4A CTD or the highly related ROC1-CUL1 CTD at 83 nM or 9.4 μM, respectively.
    KH-4-43
  • HY-16664
    SJ-172550
    		Inhibitor 99.95%
    SJ-172550 is a small molecule inhibitor of MDMX; competes for the wild type p53 peptide binding to MDMX with an EC50 of 5 μM.
    SJ-172550
  • HY-145733
    DI-1859
    		Inhibitor 99.62%
    DI-1859 is a potent, selective and covalent inhibitor of DCN1. DI-1859 inhibits neddylation of cullin 3 in cells at low nanomolar concentrations. DI-1859 induces a robust increase of NRF2 protein, a CRL3 substrate, in mouse liver and effectively protects mice from acetaminophen-induced liver damage.
    DI-1859
  • HY-149316
    Smurf1-IN-1
    		Inhibitor 99.47%
    Smurf1-IN-1 is an orally active and selective inhibitor of specific E3 ubiquitin protein ligase 1 (SMURF1) with an IC50 of 92 nM. Smurf1-IN-1 has significant efficacy in rats model of pulmonary hypertension.
    Smurf1-IN-1
  • HY-134594
    SENP1-IN-1
    		Inhibitor 99.55%
    SENP1-IN-1 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 29. SENP1-IN-1 is developed for tumor radiosensitivity enhancement.
    SENP1-IN-1
  • HY-123578
    NSC689857
    		Inhibitor 99.65%
    NSC689857 is a potent EGFR and SCFSKP2 inhibitor with an IC50 value of 36 μM for Skp2-Cks1. NSC689857 can inhibit p27 ubiquitylation (IC50=30 μM). NSC689857 has varied activity across cancer types, with more activity against leukemia cell lines than others.
    NSC689857
  • HY-153937
    Skp2 inhibitor 2
    Skp2 inhibitor 2 (14f) is an inhibitor of F-box protein S-phase kinase-associated protein 2 (Skp2), with an IC50 value of 10.2 μM (Skp2-Cks1). Skp2 is a part of cullin-RING ligases, which recruits and ubiquitinates substrates, involving in proteolytic and non-proteolytic process.
    Skp2 inhibitor 2
  • HY-120086
    RO-5963
    		Inhibitor 99.97%
    RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively.
    RO-5963
  • HY-155120
    Cbl-b-IN-5
    		Inhibitor 99.61%
    Cbl-b-IN-5 (compound 6) is a Cbl-b inhibitor (IC50=3-10 µM). Cbl-b-IN-5 has the potential to be used in the study of cancer and related diseases amenable to immune system modulation.
    Cbl-b-IN-5
  • HY-139662
    HB007
    		Inhibitor 99.73%
    HB007 is a small ubiquitin-related modifier 1 (SUMO1) degrader. HB007 induces ubiquitination and degradation of SUMO1, resulting in reduced tumor growth in vivo. HB007 can be used for the research of brain, breast, colon, and lung cancers.
    HB007
  • HY-153178
    HECT E3-IN-1
    		Inhibitor 99.43%
    HECT E3-IN-1 (compound 3) is a HECT E3 ligase inhibitor. HECT E3-IN-1 (compound 3) disrupts Ub binding to the noncovalent Ub-binding site of Nedd4-1.
    HECT E3-IN-1
  • HY-15301
    CC0651
    		Inhibitor 99.03%
    CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27Kip1, as confirmed by dose-response analysis.
    CC0651
  • HY-W176629
    Hydrocotarnine
    		Inhibitor 99.59%
    Hydrocotarnine is a Cbl inhibitor, and results in inflammasome-mediated IL-18 secretion in colitis. Hydrocotarnine increases expression of GLUT1 and cellular glucose uptake in glycolytic metabolism. Hydrocotarnine acts as an agent that provides analgesic effect in cancer research.
    Hydrocotarnine
  • HY-134596
    SENP1-IN-3
    		Inhibitor 99.92%
    SENP1-IN-3 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 17. SENP1-IN-3 is developed for tumor radiosensitivity enhancement.
    SENP1-IN-3
  • HY-101266B
    Milademetan tosylate hydrate
    		Inhibitor 98.89%
    Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis.
    Milademetan tosylate hydrate
  • HY-126075A
    WS-383
    		Inhibitor 99.88%
    WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
    WS-383
  • HY-156395
    MN551
    		Inducer 98.05%
    MN551 is a potent inhibitor of cysteine-directed electrophilic covalent that plays important roles in the biology of SOCS2 and its CRL5 complex, and as E3 ligase handles in proteolysis targeting chimera (PROTACs) to induce targeted protein degradation.
    MN551
  • HY-153775
    UC-764864
    		Inhibitor 99.85%
    UC-764864 is a UBE2N inhibitor. UC-764864 inhibits UBE2N enzymatic activity. UC-764864 has cytotoxic effects and inhibition of UBE2N-dependent signaling in leukemic cells. UC-764864 blocks ubiquitination of innate immune- and inflammatory-related substrates in human AML cell lines.
    UC-764864
  • HY-100383
    BH3I-1
    		Inhibitor ≥98.0%
    BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.
    BH3I-1
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity