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-163194
    Cbl-b-IN-16
    		Inhibitor
    Cbl-b-IN-16 (compound 31) is an orally active Cbl-b inhibtor with IC50 of 30 nM and induces IL-2 production in Hu-T-cells with EC50 of 230 nM. Cbl-b-IN-16 exhibits antitumor activity.
    Cbl-b-IN-16
  • HY-142692
    DCN1-UBC12-IN-3
    		Inhibitor
    DCN1-UBC12-IN-3 is potent and selective DCN1-UBC12 inhibitor with an IC50 of 2.25 nM. Anticardiac fibrotic effect.
    DCN1-UBC12-IN-3
  • HY-156765
    Cbl-b-IN-9
    		Inhibitor
    Cbl-b-IN-9 (Compound 300) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 5.6 nM and 4.7 nM, respectively.
    Cbl-b-IN-9
  • HY-156769
    Cbl-b-IN-13
    		Inhibitor
    Cbl-b-IN-13 (Example 520) is a Cbl-b inhibitor with an IC50 of <100 nM. Cbl-b-IN-13 has the ability to activate T-cells.
    Cbl-b-IN-13
  • HY-122210
    T521
    		Inhibitor
    T521 is an inhibitor of E3 ligase. T521 can be used in cancer and metabolic disease related research.
    T521
  • HY-159601
    CSN5-IN-1
    CSN5-IN-1 (compound Ac-11) is an inhibitor of CSN5, with IC50 values of 12.56 μM and 19 μM as measured by FP assay and fluorescence assay, respectively. CSN5-IN-1 can also downregulate the expression of PD-L1 and upregulate the expression of NEDD8-Cul1 in cells.
    CSN5-IN-1
  • HY-170430
    HGC652
    		Ligand
    HGC652 is the molecular glue, that targets E3 ubiquitin ligase TRIM21, promotes the formation of a ternary complex between TRIM21 and NUP98, induces degradation of NUP155 and nuclear pore complex proteins, thereby causing the cell death. HGC652 inhibits the proliferation of multi cancer cells, according to the expression level of TRIM21.
    HGC652
  • HY-167673
    RNF5-IN-1
    		Degrader
    RNF5-IN-1 (FX12) is a selective RNF5 degrader. RNF5-IN-1 binds to RNF5 and inhibits its E3 activity, and promotes proteasomal degradation of RNF5 in an endoplasmic reticulum (ER)-associated degradation (ERAD) way in cells. RNF5-IN-1 inhibits α-1-antitrypsin (NHK) dislocation with an IC50 value of 2.7 μM. RNF5-IN-1 can be used for research of cystic fibrosis, acute myeloid leukemia, and certain viral infections.
    RNF5-IN-1
  • HY-169968
    E3 ligase Ligand 41
    E3 ligase Ligand 41 (Compound SI-13) is a ligand for E3 ubiquitin ligase DCAF16. E3 ligase Ligand 41 can be connected to SLF (HY-114872) by a linker (HY-W040168) to form KB03-SLF (HY-147196).
    E3 ligase Ligand 41
  • HY-P3708
    TRAF6 control peptide
    		Control
    TRAF6 control peptide is a control peptide for TRAF6.
    TRAF6 control peptide
  • HY-12734
    AM-8735
    		Inhibitor
    AM-8735 is a potent and selective MDM2 inhibitor with an IC50 of 25 nM.
    AM-8735
  • HY-158706
    SAE-IN-2
    		Inhibitor
    SAE-IN-2 (compound 6) is a potent inhibitor of sumo activating enzume (SAE), with the IC50 of 27.8 nM.
    SAE-IN-2
  • HY-122615A
    SPOP-IN-6b hydrochloride
    		Inhibitor
    SPOP-IN-6b hydrochloride is a potent speckle-type POZ protein (SPOP) inhibitor with an IC50 of 3.58 μM.
    SPOP-IN-6b hydrochloride
  • HY-158172
    Cbl-b-IN-18
    		Inhibitor
    Cbl-b-IN-18 (compound 51) is an inhibitor of the E3 ligase Casitas B-lineage lymphoma proto-oncogene B (CPL-B). Cbl-b-IN-18 inhibits the phosphorylation of CPL-B (IC50< 100 nM).
    Cbl-b-IN-18
  • HY-122874
    DI-404
    		Inhibitor
    DI-404 is a potent inhibitor of DCN1 with a KKd value of 6.7 nM. DI-404 selectively inhibits neddylation of cullin 3 in a dose-dependent manner.
    DI-404
  • HY-145452
    5-Octyl-α-ketoglutarate
    		Inhibitor
    5-Octyl-α-ketoglutarate (5-Octyl 2-oxopentanedioate) is a cell-permeable substrate for lysine demethylase. 5-Octyl-α-ketoglutarate is related to protein demethylation, inhibits cell proliferation of wtCRBN expressing cells, and also enhances Lenalidomide (HY-A0003)-induced sensitivity and inhibits myeloma (MM) ) drug resistance of cells. When myeloma (MM) cells undergo glutamine-dependent proliferation, α-ketoglutarate increases glutamine catabolism to promote protein demethylation.
    5-Octyl-α-ketoglutarate
  • HY-169796
    Panepophenanthrin
    		Inhibitor
    Panepophenanthrin is a compound that can be isolated from the mushroom strain, Panus rudis Fr. IFO 8994. Panepophenanthrin is a ubiquitin-activating enzyme inhibitor.
    Panepophenanthrin
  • HY-W751400
    Solasodine hydrochloride
    		Inhibitor
    Solasodine (Purapuridine) hydrochloride is a steroidal alkaloid that occurs in plants of the Solanaceae family. Solasodine hydrochloride induces apoptosis by inhibiting the p53-MDM2 complex, p21Waf1/Cip1, and Bcl-2 proteins. Solasodine hydrochloride has neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic and anti-inflammatory activities.
    Solasodine hydrochloride
  • HY-W004883
    3-Amino-4,6-dimethylpyridine
    		Inhibitor 99.87%
    3-Amino-4,6-dimethylpyridine (5A-DMP) is a UHRF1 inhibitor that targets the Arg-binding cavity site within the UHRF1 TTD domain. 3-Amino-4,6-dimethylpyridine disrupts the interaction between UHRF1 and LIG1, interfering with DNA methylation, and can be utilized in cancer research.
    3-Amino-4,6-dimethylpyridine
  • HY-18327
    HLI98C
    		Inhibitor
    HLI98C is a ubiquitin ligase inhibitor. HLI98C inhibits p53 ubiquitylation. HLI98C inhibits HDM2 auto-ubiquitylation.
    HLI98C
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity