GLPBio

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.

Products Related to E1/E2/E3 Enzyme(113)

  • GC65305 structure
    GC65305BI8622
    CAS: 1875036-74-0
    Purity: >99.00%

    BI8622 is a specific inhibitor of the ubiquitin ligase HUWE1 with an IC50 of 3.1 μM.

  • GC65469 structure
    GC65469SENP1-IN-1
    CAS: 2416910-69-3
    Purity: >98%

    SENP1-IN-1 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 29. SENP1-IN-1 is developed for tumor radiosensitivity enhancement.

  • GC65576 structure
    GC65576DI-1859
    CAS: 2247061-09-0
    Purity: >98%

    DI-1859 is a potent, selective and covalent inhibitor of DCN1.

  • GC65605 structure
    GC65605RB-3
    CAS: 2396639-11-3
    Purity: >98.00%

    RB-3, a PRC1 inhibitor, binds to RING1B-BMI1f, with a Kd of 2.8 μM.

  • GC65881 structure
    GC65881Teslexivir hydrochloride
    CAS: 1075281-70-7
    Purity: >99.00%

    Teslexivir (BTA074) hydrochloride is a potent antiviral agent. Teslexivir hydrochloride is a potent and selective inhibitor of the interaction between two essential viral proteins, E1 and E2, an association that is a necessary step in the DNA replication and thus viral production for Human Papilloma Virus (HPV) 6 and 11. Teslexivir hydrochloride can be used for condyloma research.

  • GC68150 structure
    GC68150BC-1382
    CAS: 1013753-99-5
    Purity: >99.00%
  • GC68840 structure
    GC68840Cbl-b-IN-3
    CAS: 2573775-59-2
    Purity: >99.00%

    Cbl-b-IN-3 (Compound 23) is an inhibitor of Casitas B-lineage lymphoma proto-oncogene b (Cbl-b), with an IC50 of

  • GC69217 structure
    GC69217HECT E3-IN-1
    CAS: 1810058-52-6
    Purity: >99.00%

    HECT E3-IN-1 (compound 3) is an inhibitor of HECT E3 ligase. HECT E3-IN-1 (compound 3) disrupts the non-covalent binding site of Ub with Nedd4-1.

  • GC69842 structure
    GC69842Rugonersen
    CAS: 2591587-57-2
    Purity: >91.00%

    Rugonersen (RG6091; RO7248824) is an antisense oligonucleotide (ASO) modified with locked nucleic acid (LNA), which reduces the silencing of ubiquitin protein ligase E3A (UBE3A). Angelman syndrome (AS) is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A. Rugonersen has been used in research on AS.

  • GC69866 structure
    GC69866SCFSkp2-IN-2
    CAS: 1375060-02-8
    Purity: >99.00%

    SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a KD of 28.77 μM. AAA-237 induces apoptosis in NSCLC cells and exhibits anti-tumor activity.

  • GC69911 structure
    GC69911Skp2 inhibitor 1
    CAS: 2760612-63-1
    Purity: >99.00%

    Skp2 inhibitor 1 (compound 14i) is a Skp2 inhibitor that disrupts the Skp2-Cks1 interaction, with an IC50 of 2.8 μM. Skp2 inhibitor 1 also exhibits anti-cancer activity.

  • GC70082 structure
    GC70082UBA5-IN-1
    CAS: 1831169-11-9
    Purity: >98.00%

    UBA5-IN-1 (compound 8.5) is a selective inhibitor of UBA5 with an IC50 value of 4.0 μM. UBA5-IN-1 inhibits the proliferation of Sk-Luci6 cancer cells that overexpress UBA5.

  • GC71320 structure
    GC71320Cbl-b-IN-5
    CAS: 2368835-59-8
    Purity: >99.00%

    Cbl-b-IN-5 (compound 6) is a Cbl-b inhibitor (IC50=3-10 µM).

  • GC73155 structure
    GC73155Rugonersen sodium
    CAS: 2591588-58-6
    Purity: >91.00%

    Rugonersen sodium is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing.

  • GC73229 structure
    GC73229Smurf1-IN-1
    CAS: 1824708-03-3
    Purity: >99.00%

    Smurf1-IN-1 is an orally active and selective inhibitor of specific E3 ubiquitin protein ligase 1 (SMURF1) with an IC50 of 92 nM.

  • GC73363 structure
    GC73363Antitumor agent-81
    CAS: 2765180-17-2
    Purity: >98.00%

    Antitumor agent-81 (compound 5a) is a low cytotoxicity P62-RNF168 agonist that enhances the interaction between P62 and RNF168.

  • GC73485 structure
    GC73485UC-764864
    CAS: 278806-03-4
    Purity: >99.00%

    UC-764864 is a UBE2N inhibitor.

  • GC73512 structure
    GC73512Skp2 inhibitor 2
    CAS: 2760612-77-7

    Skp2 inhibitor 2 (14f) is an inhibitor of F-box protein S-phase kinase-associated protein 2 (Skp2), with an IC50 value of 10.2 μM (Skp2-Cks1).

  • GC73748 structure
    GC73748PELI1-IN-1
    Purity: >98.00%

    PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase.

  • GC73800 structure
    GC73800MS181
    Purity: >98.00%

    MS181 (compound 1) is a potent cereblon (CRBN)-recruiting and EED-binding polycomb repressive complex 1 (PRC1) PROTAC degrader.

  • GC73900 structure
    GC73900HA-9104
    CAS: 2412367-83-8
    Purity: >98.00%

    HA-9104 is a potent and selective inhibitor of cullin-5 neddylation via virtually targeting the V30 pocket of UBE2F.

  • GC74157 structure
    GC74157EN450
    CAS: 793719-01-4
    Purity: >99.00%

    EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB.

  • GC79075 structure
    GC79075NVS1.1
    Purity: >98%

    NVS1.1 is an orally active, blood-brain barrier-penetrant eRF1 degrader.

  • GC79626 structure
    GC79626H111-H7
    CAS: 220965-54-8
    Purity: >98.00%

    H111-H7 is a WW domain containing E3 ubiquitin 27 protein ligase 2 ( WWP2 ) inhibitor with a K D of 717 nM.