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-D2259
    PFI-7
    PFI-7 is a probe, which binds to human GID4 (KD is 79 nM), and antagonizes the binding of Pro/N-degrons. PFI-7 can be utilized in C-terminal to LisH (CTLH) complex research and development of targeted protein degradation.
    PFI-7
  • HY-178458
    UBA5-IN-2
    		Inhibitor
    UBA5-IN-2 (Compound 50) is a potent ubiquitin-like modifier activating enzyme 5 (UBA5) inhibitor (IC50=0.063 μM). UBA5-IN-2 is promising for research of cancers and protein homeostasis-related diseases.
    UBA5-IN-2
  • HY-100765
    BI-0252
    		Inhibitor
    BI-0252 is an orally active, selective MDM2-p53 inhibitor with an IC50 of 4 nM. BI-0252 can induce tumor regressions in all animals of a mouse SJSA-1 xenograft, with concomitant induction of the tumor protein p53 (TP53) target genes and markers of apoptosis.
    BI-0252
  • HY-185652
    dTAG-TRIMTAC
    		Ligand
    dTAG-TRIMTAC is a PROTAC-like degrader targeting TRIM21. dTAG-TRIMTAC forms a ternary complex with TRIM21 and target proteins to drive degradation of oligomeric/assembled substrates via TRIM21 clustering-based activation, with degradation dependent on endogenous TRIM21. dTAG-TRIMTAC can be used for the research of neurodegenerative disease and inflammatory disease.
    dTAG-TRIMTAC
  • HY-178518
    Thalidomide-C1-O-CO-C2-Piperazine-CO-C1-Azacyclohexane-C1-Piperazine
    Thalidomide-C1-O-CO-C2-Piperazine-CO-C1-Azacyclohexane-C1-Piperazine is an E3 ligase ligand-linker conjugate containing a cereblon (CRBN) ligand for E3 ubiquitin ligase and a linker. Thalidomide-C1-O-CO-C2-Piperazine-CO-C1-Azacyclohexane-C1-Piperazine can be used to synthesize PROTAC CDK4/6/9 degrader 2 (HY-178516).
    Thalidomide-C1-O-CO-C2-Piperazine-CO-C1-Azacyclohexane-C1-Piperazine
  • HY-P11621
    JWP24
    		Inhibitor
    JWP24 is the first cell membrane-permeable peptide inhibitor of MAGE-A4, with an IC50 of 200 nM against human MAGE-A4. JWP24 binds to intracellular targets while retaining binding activity, disrupts the interaction between MAGE-A4 and RAD18, and does not induce cytotoxicity at effective concentrations. JWP24 is applicable for cancer-related research.
    JWP24
  • HY-156763
    Cbl-b-IN-7
    		Inhibitor
    Cbl-b-IN-7 (Compound 248) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 6.7 nM and 5.2 nM, respectively.
    Cbl-b-IN-7
  • 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-183997
    Cbl-b-IN-33
    		Inhibitor
    Cbl-b-IN-33 is an orally active, selective inhibitor of Casitas B-lineage lymphoma-b (Cbl-b) with an IC50 of 7 nM and a Kd of 1.2 nM. Cbl-b-IN-33 inhibits non-phosphorylated E3 ubiquitin ligase Cbl-b, induces IL-2 activation in peripheral blood mononuclear cells, and exerts tumor growth inhibitory effects in a mouse colon cancer model. Cbl-b-IN-33 can be used for the research of colon cancer.
    Cbl-b-IN-33
  • HY-183638
    T7117
    		Inhibitor
    T7117 is a TRIM25-HIF-1α inhibitor. T7117 disrupts the interaction between TRIM25-HIF-1α. T7117 can be used for the research of glioblastoma.
    T7117
  • HY-177651B
    Obudanersen sodium scrambled negative control
    		Inhibitor
    Obudanersen sodium scrambled negative control is the sequence scrambled negative control of Obudanersen sodium.
    Obudanersen sodium scrambled negative control
  • 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-164133
    SM00465
    		Inhibitor
    SM00465 (Compound 207) is a Cbl-b inhibitor-linker conjugate composed of INT4 (HY-179262) and Linker (HY-179263). SM00465 can be used for ADC synthesis. SM00465 is applicable to the research of immune-related diseases.
    SM00465
  • 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-170515A
    (E),(Z)-RNF5 agonist 1
    		Agonist
    (E),(Z)-RNF5 agonist 1 (Compound Analog-1) is a RNF5 agonist that can enhance the ubiquitination and degradation of SARS-CoV-2 E protein by RNF5. (E),(Z)-RNF5 agonist 1 effectively inhibits the replication of SARS-CoV-2 and significantly alleviates pulmonary pathological damage and systemic inflammatory response in mouse infection models. (E),(Z)-RNF5 agonist 1 has a strong cytotoxic effect on neuroblastoma and melanoma. (E),(Z)-RNF5 agonist 1 can be used for research on anti-cancer and anti-viral purposes.
    (E),(Z)-RNF5 agonist 1
  • HY-179617
    Cbl-b-IN-30
    		Inhibitor
    Cbl-b-IN-30 is an orally active Casitas B-lineage lymphoma-b (CBLB) inhibitor. Cbl-b-IN-30 specifically binds to CBLB and inhibits its E3 ubiquitin ligase activity with an IC50 of 9.1 nM. Cbl-b-IN-30 can promote IL-2 secretion (EC50 = 187.5 nM) and enhance T cell activation. Cbl-b-IN-30 exerts antitumor activity and can induce immune memory. Cbl-b-IN-30 can be used for the research of colon cancer.
    Cbl-b-IN-30
  • HY-P992297
    Anti-RNF43 Antibody
    Anti-RNF43 Antibody is a monoclonal antibody targeting RNF43. It can be used in ELISA, FACS, and functional assays. For isotype controls of Anti-RNF43 Antibody, please refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-RNF43 Antibody
  • HY-180108
    H111-H7
    		Inhibitor 98.14%
    H111-H7 is a WW domain containing E3 ubiquitin 27 protein ligase 2 (WWP2) inhibitor with a KD of 717 nM. H111-H7 inhibits WWP2 expression, restores the succinate dehydrogenase complex subunit C (SDHC) level, and defers the acute kidney injury (AKI)-to-chronic kidney disease (CKD) transition in unilateral kidney ischemia–reperfusion (UIR) mice. H111-H7 can be used for AKI-to-CKD transition research.
    H111-H7
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Cat. No. Product Name / Synonyms Application Reactivity