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-135844
    LS-102
    		Inhibitor
    LS-102 is a selective E3 ubiquitin ligase synoviolin (Syvn1) inhibitor. LS-102 inhibits the autoubiquitination of synoviolin with an IC50 of 35 μM. LS-102 has the potential for rheumatoid arthritis treatment.
    LS-102
  • HY-N0077
    Ginkgolic Acid
    		Inhibitor 99.65%
    Ginkgolic Acid is a natural compound that inhibits SUMOylation with an IC50 of 3.0 μM in in vitro assay.
    Ginkgolic Acid
  • HY-18658
    Siremadlin
    		Inhibitor 99.87%
    Siremadlin (NVP-HDM201) is a potent, orally bioavailable and highly specific p53-MDM2 interaction inhibitor.
    Siremadlin
  • HY-19817
    PRT4165
    		Inhibitor ≥98.0%
    PRT4165 is a potent inhibitor of polycomb-repressive complex 1 (PRC1)-mediated H2A ubiquitylation.
    PRT4165
  • HY-13811
    NSC697923
    		Inhibitor 99.93%
    NSC697923 is a potent UBE2N (ubiquitin-conjugating enzyme E2 N, Ubc13) inhibitor. NSC697923 induces neuroblastoma (NB) cell death via promoting nuclear importation of p53 in p53 wild-type NB cells. NSC697923 also induces cell death in p53 mutant NB cells by activation of JNK-mediated apoptotic pathway. NSC697923 inhibits DNA damage and NF-κB signaling. Antitumor activity.
    NSC697923
  • HY-101266
    Milademetan
    		Inhibitor 98.87%
    Milademetan (DS-3032) is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) induces G1 cell cycle arrest, senescence and apoptosis.
    Milademetan
  • HY-120929
    BI8622
    		Inhibitor 98.28%
    BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM.
    BI8622
  • 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.
    RG7112
  • HY-100237
    SZL P1-41
    		Inhibitor 99.92%
    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.
    SZL P1-41
  • HY-101518
    Alrizomadlin
    		Inhibitor 98.67%
    Alrizomadlin (APG-115) is an orally active MDM2 protein inhibitor binding to MDM2 protein with IC50 and Ki values of 3.8 nM and 1 nM, respectively. Alrizomadlin blocks the interaction of MDM2 and p53 and induces cell-cycle arrest and apoptosis in a p53-dependent manner.
    Alrizomadlin
  • HY-141432
    NX-1607
    		Inhibitor 99.42%
    NX-1607 (Compound 23) is an inhibitor of Cbl-b, an E3 enzyme in the ubiquitin-proteasome pathway, with an IC50 value of less than 1 nM. NX-1607 can be used in cancer research.
    NX-1607
  • HY-103236
    NSC232003
    		Inhibitor 99.27%
    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.
    NSC232003
  • HY-16661
    Skp2 Inhibitor C1
    		Inhibitor 98.21%
    Skp2 Inhibitor C1 (SKPin C1) is an S-phase kinase-related protein 2 (Skp2) inhibitor with an inhibitory effect on metastatic melanoma cells. Skp2 Inhibitor C1 slows the cell cycle, inhibits cell proliferation, and triggers apoptosis.
    Skp2 Inhibitor C1
  • HY-136339
    Cbl-b-IN-1
    		Inhibitor 99.68%
    Cbl-b-IN-1 (example 519) is a Cbl-b inhibitor, extracted from patent WO2019148005A1, with an IC50 <100 nM.
    Cbl-b-IN-1
  • HY-101836
    DKM 2-93
    		Inhibitor 98.76%
    DKM 2-93 is a relatively selective inhibitor of UBA5 with an IC50 of 430 μM.
    DKM 2-93
  • HY-100507
    Avadomide
    		Agonist 99.14%
    Avadomide is an orally active cereblon modulator. Avadomide 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 exhibits potent antitumor and immunomodulatory activities.
    Avadomide
  • HY-120204
    BI8626
    		Inhibitor 99.20%
    BI8626 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 0.9 μM.
    BI8626
  • HY-152859
    Brigimadlin
    		Inhibitor 99.72%
    Brigimadlin (BI 907828) is an orally active E3 ubiquitin-protein ligase MDM-2 inhibitor, preventing MDM-2 from negatively regulating the tumor suppressor p53. Brigimadlin can be used for antineoplastic research.
    Brigimadlin
  • HY-N2360
    Hinokiflavone
    		Inhibitor 99.80%
    Hinokiflavone is a novel modulator of pre-mRNA splicing activity extracted from plants with anti-inflammatory, anti-tumor and antiviral activities. Hinokiflavone is also a potent inhibitor for matrix metalloproteinases (MMPs). Hinokiflavone attenuates the virulence of Methicillin (HY-121544)-resistant staphylococcus aureus by inhibiting caseinolytic protease P (ClpP) with an IC50 value of 34.36 mg/mL. Hinokiflavone induces apoptosis via the reactive oxygen species-mitochondria-mediated apoptotic pathway and inhibits tumor cell migration and invasion. Hinokiflavone is a SUMO protease inhibitor against sentrin-specific protease 1 (SENP1) activity.
    Hinokiflavone
  • HY-12025
    Serdemetan
    		Inhibitor 99.81%
    Serdemetan (JNJ-26854165) is a potent anticancer agent with radiosensitizing activity. Serdemetan exhibits antiproliferative activity in various p53 wild-type tumor cells. Serdemetan also antagonizes the Mdm2-HIF1α axis leading to decreased levels of glycolytic enzymes.
    Serdemetan
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity