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-163576
    GID4-IN-1
    		Inhibitor
    GID4-IN-1 (compd 169) is a GID4 inhibitor with an IC50 <500 nM.
    GID4-IN-1
  • HY-168964
    Ethanolamine-Thalidomide-4-OH
    Ethanolamine-Thalidomide-4-OH is an E3 Ligase Ligand-Linker Conjugate composed of an CRBN ligand (HY-103596) and a linker (HY-Y0524), and can be used for synthesis of PROTACs (eg: PROTAC BTK Degrader-13 (HY-168963)).
    Ethanolamine-Thalidomide-4-OH
  • 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-177615A
    Apazunersen sodium
    		Inhibitor
    Apazunersen sodium is an antisense oligonucleotide (ASO) that targets and inhibits expression of the UBE3A antisense transcript (UBE3A-AS) to prevent silencing of the paternally inherited allele of the UBE3A gene and reactivate expression of the deficient
    Apazunersen sodium
  • 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-156661
    MurF-IN-1
    		Inhibitor 98.0%
    MurF-IN-1 (Compound 7) is a MurF inhibitor with an pIC50 of 5.19 against S. pneumoniae MurF.
    MurF-IN-1
  • HY-123888
    Viomellein
    		Inhibitor
    Viomellein is a SUMOylation inhibitor with antibacterial and anticancer activities. Viomellein inhibits biofilm formation of strains produced from the fungus Aspergillus ochraceus from the Mediterranean sponge Agelas oroides. Viomellein exhibits cytotoxicity against A2780 human ovarian cancer cells with an IC50 value of 5.0 μM. Viomellein also inhibits SUMOylation of RanGAP1 (GTPase activating protein) with an IC50 of 10.2 μM.
    Viomellein
  • 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-173311
    Cbl-b-IN-28
    		Inhibitor
    Cbl-b-IN-28 (Compound B2) is an orally active Cbl-b inhibitor. Cbl-b-IN-28 promotes the secretion of cytokines such as IL-2 and enhances the function of immune cells by regulating the phosphorylation levels of key proteins in the T-cell receptor signaling pathway. Cbl-b-IN-28 can be used in research in the field of cancer immunology.
    Cbl-b-IN-28
  • HY-176907
    ML-93
    		Inhibitor
    ML-93 is an orally active SAE inhibitor, with an IC50 value of 0.4 μM. ML-93 inhibits the SUMOylation pathway in HCT116 cells. ML-93 shows robust antitumor activity in the HCT116 colorectal carcinoma xenograft model. ML-93 can be used for the study of colorectal cancer.
    ML-93
  • HY-172595
    Apoptosis inducer 48
    		Agonist
    Apoptosis inducer 48 (5d) is an apoptotic agent. Apoptosis inducer 48 inhibits the growth of triple-negative breast cancer cells. Apoptosis inducer 48 attenuates proteasomal degradation via the ubiquitin-proteasome pathway, leading to G2/M phase cell cycle arrest and the induction of apoptotic.
    Apoptosis inducer 48
  • HY-P11020
    p27 Analogue CP2
    		Inhibitor
    p27 Analogue CP2 is a macrocyclic peptide inhibitor targeting the SCFSkp2/Cks1 E3 ubiquitin ligase (Kd=32 nM). p27 Analogue CP2 blocks SCFSkp2/Cks1-mediated ubiquitylation and degradation of p27, restoring p27 levels and inhibiting cell proliferation. p27 Analogue CP2 is promising for research of cancers dependent on Skp2 overexpression such as breast cancer.
    p27 Analogue CP2
  • 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-174853
    TRIM25 ligand-1
    		Ligand
    TRIM25 ligand-1 (Compound 10) is a covalent ligand. TRIM25 ligand-1 can covalently bind to Cys498 in the PRYSPRY domain of TRIM25 and enhance its auto-ubiquitination activity. TRIM25 ligand-1 is selective for TRIM25 in vitro and in live cells.
    TRIM25 ligand-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-177651A
    Obudanersen sodium
    		Inhibitor
    Obudanersen sodium is an antisense oligonucleotide targeted to ubiquitin protein ligase E3A-antisense transcript (UBE3A-ATS). It is used for the study of Angelman syndrome.
    Obudanersen sodium
  • 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-175861
    NSC20116
    		Inhibitor
    NSC20116 is a uracil derivative that specifically targets the Set-and-Ring (SRA) domain of the oncogene UHRF1. NSC20116 binds to the 5-methylcytosine (5mC) (HY-W008091) recognition pocket of UHRF1 SRA domain, with a dissociation constant (Kd) of 362 nM. NSC20116 can be used for the study of cancer.
    NSC20116
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity