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-134595
    SENP1-IN-2
    		Inhibitor
    SENP1-IN-2 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 30. SENP1-IN-2 is developed for tumor radiosensitivity enhancement.
    SENP1-IN-2
  • HY-131667
    Hdm2 E3 ligase inhibitor 1
    		Inhibitor
    Hdm2 E3 ligase inhibitor 1 (Compound 1) is a reversible inhibitor for Hdm2 (an E3 ubiquitin ligase)-mediated ubiquitination of the p53 protein with an IC50 of 12.7 μM. Hdm2 E3 ligase inhibitor 1 binds Hdm2, blocks Hdm2-catalyzed ubiquitin transfer from preligated Ub-Ubc4 to p53, inhibits p53 ubiquitination, stabilizes p53 protein in tumor cell and exhibits antitumor efficacy.
    Hdm2 E3 ligase inhibitor 1
  • HY-156373
    MN714
    		Inhibitor
    MN714 is a pivaloyloxymethyl (POM) protected inhibitor.
    MN714
  • HY-158171
    Cbl-b-IN-17
    		Inhibitor
    Cbl-b-IN-17 (Example-40) is an inhibitor of Cbl-b with an IC50 value <100 nM.
    Cbl-b-IN-17
  • HY-151358
    SENP2-IN-1
    		Inhibitor
    SENP2-IN-1 (compound 77) is a selective SENP2 inhibitor. SENP2-IN-1 shows inhibitory activities with IC50s of 1.3, 0.69 and 22.7 μM for SENP1, SENP2 and SENP5, respectively. SENP2-IN-1 can be used for the research of cancer.
    SENP2-IN-1
  • HY-12296S
    Navtemadlin-d7
    		Inhibitor
    Navtemadlin-d7 is the deuterium labeled Navtemadlin. Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM[1][2].
    Navtemadlin-d<sub>7</sub>
  • HY-163809
    BRD9 Degrader-2
    BRD9 Degrader-2 (Compound B11) is a BRD9 degrader (DC50 ≤1.25 nM; Dmax≥75%). BRD9 Degrader-2 can be used for research of cancers.
    BRD9 Degrader-2
  • HY-156764
    Cbl-b-IN-8
    		Inhibitor
    Cbl-b-IN-8 (Compound 293) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 5.5 nM and 7.8 nM, respectively.
    Cbl-b-IN-8
  • HY-155477
    Cbl-b-IN-15
    		Inhibitor
    Cbl-b-IN-15 (compound 25) is an inhibitor of the RING finger E3 ligase Cbl (IC50: 15 nM). Cbl-b refers to Casitas B-lineage lymphoma proto-oncogene-b, which inhibits T-cell, natural killer (NK) cell, and B-cell activation. Cbl-b-IN-15 activates T cell function with EC50=0.41 μM.
    Cbl-b-IN-15
  • HY-156767
    Cbl-b-IN-11
    		Inhibitor
    Cbl-b-IN-11 (Compound 466) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 6.4 nM and 6.1 nM, respectively.
    Cbl-b-IN-11
  • HY-163639
    BRD4 degrader-2
    BRD4 degrader-2 (Compound JP-2-197) is a covalent monovalent molecular glue BRD4degrader that induces a ternary complex formation between BRD4 and RNF126. BRD4 degrader-2 targets RNF126 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells.
    BRD4 degrader-2
  • HY-163641
    AR Degrader-1
    AR Degrader-1 (Compound ML 2-9) is a molecular glue androgen receptor (AR) monovalent degrader. AR Degrader-1 degrades AR through DCAF16 (E3 ligase) without obvious cytotoxicity in LNCaP prostate cancer cells.
    AR Degrader-1
  • HY-144099
    Keap1-Nrf2-IN-4
    		Inhibitor
    Keap1-Nrf2-IN-4 is a potent neddylation inhibitor. Keap1-Nrf2-IN-4 exhibits potent anti-proliferation activity against MGC-803 cells (IC50=2.55 µM). Keap1-Nrf2-IN-4 blocks the migration ability and induces apoptosis of gastric cancer cells. Keap1-Nrf2-IN-4 inhibits tumor growth without obvious toxicity.
    Keap1-Nrf2-IN-4
  • HY-N0077R
    Ginkgolic Acid (Standard)
    		Inhibitor
    Ginkgolic Acid (Standard) is the analytical standard of Ginkgolic Acid. This product is intended for research and analytical applications. Ginkgolic Acid is a natural compound that inhibits SUMOylation with an IC50 of 3.0 μM in in vitro assay.
    Ginkgolic Acid (Standard)
  • HY-125660
    Leucettamol A
    		Inhibitor
    Leucettamol A is an inhibitor of Ubc13 (ubiquitin E2 enzyme)-Uev1A interaction, with an IC50 of 50 μg/mL. Leucettamol A can potentially activate the expression of cancer suppressor p53 and is a precursor of anticancer agents. Leucettamol A can be isolated from a marine sponge, Leucetta aff. Microrhaphis.
    Leucettamol A
  • HY-158173
    Cbl-b-IN-19
    		Inhibitor
    Cbl-b-IN-19 (Compound 49) is an inhibitor for casitas B-lineage lymphoma b(Cbl-b), that inhibits Cbl-b phosphorylation with an IC50 < 100 nM.
    Cbl-b-IN-19
  • HY-168601
    WWP1/2-IN-1
    		Inhibitor
    WWP1/2-IN-1 (compound 11) is a WWP1/2 inhibitor with the IC50 values of 32.7µM and 269.2µM for WWP1 and WWP2, respectively.
    WWP1/2-IN-1
  • HY-163518
    Antitumor agent-153
    Antitumor agent-153 (compound 11b) is an optimized H2A histone ubiquitination inhibitor based on PRT4165 (HY-19817). Antitumor agent-153 inhibits the viability of human osteosarcoma U2OS cells and reduces histone H2A monoubiquitination, exhibiting anticancer activity.
    Antitumor agent-153
  • HY-168293
    p62-ZZ ligand 1
    p62-ZZ ligand 1 (Compound 7) is an p62-ZZ ligand. p62-ZZ ligand 1 can be used for synthesis of VinclozolinM2-2204 (HY-161741).
    p62-ZZ ligand 1
  • HY-161901
    BC-1293
    		Inhibitor
    BC-1293 is an inhibitor for E3 ligase subunit FBXO24. BC-1293 disrupts the interaction between FBXO24 and aspartyl-tRNA synthetase (DARS2) and increases the level of DARS2. BC-1293 increases levels of IL-1β, IL-9, MIP-2, and TNF α, and exhibits immunostimulatory activity in mice.
    BC-1293
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity