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-E70618
    Ubiquitin Conjugating enzyme E2C
    Ubiquitin Conjugating enzyme E2C (EC 2.3.2.24) is a member of the E2 ubiquitin-conjugating enzyme family, and it is the principal regulator of pathways for protein degradation in eukaryotes. Ubiquitin Conjugating enzyme E2C is involved in the tumorigenesis of various malignancies. Ubiquitin Conjugating enzyme E2C is also involved in mitotic cyclin disruption, affecting cell cycle progression. Ubiquitin Conjugating enzyme E2C is a prognostic indicator for cholangiocarcinoma.
    Ubiquitin Conjugating enzyme E2C
  • HY-129108
    9-cis-UAB30
    		Inhibitor
    9-cis-UAB30 is a rexinoid agonist. 9-cis-UAB30 significantly decreases the proliferation, viability, and motility of both patient-derived xenografts (PDXs). 9-cis-UAB30 induced cell-cycle arrest as demonstrated by the significant increase in the percentage of cells in G1 and a decrease in the percentage of cells in S phase by downregulating SKP2 and/or 20S proteasome activity, which leads to increased p27kip1 protein stability. 9-cis-UAB30 downregulates the abundance of stem cell marker mRNAs (Oct4, Nanog, Sox2, nestin) and upregulates the abundance of differentiation marker mRNAs (β3-tubulin, NSE, HOXC9, GAP43). 9-cis-UAB30 has no adverse effects on the central nervous system and cardiovascular system at the tested dose. 9-cis-UAB30 can be used for the study of neuroblastoma, cutaneous T-cell lymphomas, and breast cancer.
    9-cis-UAB30
  • 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-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.
    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-175187
    LO-3-63
    LO-3-63, a Ribociclib (HY-15777) analog bearing a truncated fumaramide handle, is a PROTAC-like CDK4/6 degrader. LO-3-63 induces CUL4DCAF16-dependent degradation of CDK4/6 in cells.
    LO-3-63
  • HY-168243
    E3 ligase Ligand 36
    E3 ligase Ligand 36 is an E3 ligase Ligand, and can be used for synthesis of PROTACs, such as PROTAC BRM/BRG1 degrader-1 (HY-168242).
    E3 ligase Ligand 36
  • 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-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-W342380
    SPI-05
    		Inhibitor
    SPI-05 (NSC 5067) is a non-competitive SUMO-specific proteases (SENP1/2) inhibitor (IC50=60 μM). SPI-05 is promising for research of cancers, such as prostate cancer and hypoxia-driven solid tumors with SENP1 overexpression.
    SPI-05
  • 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-170058
    CRBN ligand-12
    CRBN ligand-12 (Compound 9) is a CRBN-type E3 ubiquitin ligase ligand. CRBN ligand-12 can be used to prepare PROTACs.
    CRBN ligand-12
  • HY-176861
    Hakin-1
    		Inhibitor
    Hakin-1 is a E3 Ubiquitin-Ligase Hakai inhibitor. Hakin-1 blocks Hakai-mediated global ubiquitination and specific ubiquitination of E-cadherin and inhibits epithelial-mesenchymal transition (EMT) progression. Hakan-1 inhibits tumor progression and cancer metastasis. Hakin-1 can be used for the study of carcinoma such as colorectal cancer.
    Hakin-1
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Cat. No. Product Name / Synonyms Application Reactivity