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-158174
    Cbl-b-IN-20
    		Inhibitor
    Cbl-b-IN-20 (Example 50) is a casitas proto-oncogene-B ( CPL-B ) inhibitor with IC50 <100 nM.
    Cbl-b-IN-20
  • HY-142691
    DCN1-UBC12-IN-1
    		Inhibitor
    DCN1-UBC12-IN-1 is potent and selective DCN1-UBC12 inhibitor with an IC50 of 2.86 nM. Anticardiac fibrotic effect.
    DCN1-UBC12-IN-1
  • HY-161977
    Cbl-b-IN-26
    		Inhibitor
    Cbl-b-IN-26 (Example A1) is a Cbl-b inhibitor with a Kd of 34.6 nM . Cbl-b-IN-26 can be used in the study of chronic viral infections and cancer.
    Cbl-b-IN-26
  • HY-168602
    NSC-217913
    		Inhibitor
    NSC-217913 is an inhibitor of WWP1 with an IC50 value of 158.3 μM.
    NSC-217913
  • 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-175179
    LO-3-61
    LO-3-61, a JQ-1 (HY-13030) analog bearing a truncated fumaramide handle, is a PROTAC (proteolysis-targeting chimeras)-like BRD4 degrader. LO-3-61 degrades both the long and short isoforms of BRD4 CUL4DcAr16-dependently in cells. LO-3-61 shows selectivity for BRD3 and BRD4 degradation in MDA-MB-231 cells.
    LO-3-61
  • HY-163576
    GID4-IN-1
    		Inhibitor
    GID4-IN-1 (compd 169) is a GID4 inhibitor with an IC50 <500 nM.
    GID4-IN-1
  • HY-174346
    Skp2-IN-4
    		Inhibitor
    Skp2-IN-4 is an Skp2 inhibitor with a IC50 of 0.38  μM for Skp2-Cks1 binding. Skp2-IN-4 improves anti-tumor activity, inhibits the proliferation and induces S phase arrest by targeting Skp2. Skp2-IN-4 significantly enhances Cisplatin (HY-17394) chemosensitivity by suppressing the tumor cell stemness in NCl-H1299 xenograft mice model, promising for lung cancer and esophageal cancer research.
    Skp2-IN-4
  • 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-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-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-122210
    T521
    		Inhibitor
    T521 is an inhibitor of E3 ligase. T521 can be used in cancer and metabolic disease related research.
    T521
  • 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-172595
    Apoptotic agent-5
    		Agonist
    Apoptotic agent-5 (5d) is an apoptotic agent. Apoptotic agent-5 inhibits the growth of triple-negative breast cancer cells. Apoptotic agent-5 attenuates proteasomal degradation via the ubiquitin-proteasome pathway, leading to G2/M phase cell cycle arrest and the induction of apoptotic.
    Apoptotic agent-5
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity