2. シグナル伝達
  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

Related Products

PDF 1.36 MB

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.

製品番号 製品名 製品効果 純度 構造式
  • HY-179575
    Cbl-b-IN-29 Inhibitor
    Cbl-b-IN-29 is an orally active CBL-B inhibitor. Cbl-b-IN-29 binds to the CBL-B active pocket. Cbl-b-IN-29 induces Jurkat cell release IL-2 with an EC50 of 159 nM, effectively inhibiting the function of immune E3 ubiquitin ligase. Cbl-b-IN-29 demonstrates robust anti-tumor efficacy in vivo with good tolerability and no observed adverse reactions. Cbl-b-IN-29 can be used for cancer immunotherapy, colorectal cancer and immune-oncology combination research.
    Cbl-b-IN-29
  • 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-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-183293
    Cbl-b-IN-32 Inhibitor
    Cbl-b-IN-32 is a Cbl-b inhibitor with an IC50 of 6.83 μM. Cbl-b-IN-32 binds to the TKB-LH interface, stabilizes the inactive conformation of Cbl-b, engages Tyr363 via hydrogen bonds and water bridges, and forms hydrogen bonds with Phe261 and Phe263.
    Cbl-b-IN-32
  • HY-P11792
    CP2-CPP
    CP2-CPP is a conjugate of p27 Analogue CP2 (HY-P11020) and Antennapedia Peptide (HY-P0307). CP2-CPP crosses cell membranes and localizes to live cell cytosol. CP2-CPP blocks SCFSkp2/Cks1-p27 interaction to inhibit p27 ubiquitination and degradation, restoring p27 levels and inhibiting cell proliferation. CP2-CPP can be used for the research of cancer, such as breast cancer.
    CP2-CPP
  • 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-184150
    EN10 Ligand
    EN10 is a ligand for the muscle-specific E3 ligase KLHL41, which can be used to synthesize PROTAC KBD-1 (HY-184151) targeting BRD4.
    EN10
  • 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
  • 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-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-177651
    Obudanersen Inhibitor
    Obudanersen is an antisense oligonucleotide targeted to ubiquitin protein ligase E3A-antisense transcript (UBE3A-ATS). It is used for the study of Angelman syndrome.
    Obudanersen
  • HY-175186
    LO-3-62
    LO-3-62 is a PROTAC-like SMARCA2/4 degrader with a truncated fumaramide handle. LO-3-62 degrades SMARCA2/4 in cells.
    LO-3-62
製品番号 製品名 / Synonyms Species Source
製品番号 製品名 / Synonyms Application Reactivity