2. Metabolic Enzyme/Protease
  3. E1/E2/E3 Enzyme

E1/E2/E3 Enzyme

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.

E1/E2/E3 Enzyme Related Products (134):

Cat. No. Product Name Effect Purity
  • HY-15676
    Idasanutlin Inhibitor 99.93%
    Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM.
  • HY-111789
    Subasumstat Inhibitor 98.56%
    Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities[1][2].
  • HY-100487
    TAK-243 Inhibitor
    TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis[1][2].
  • HY-10029
    Nutlin-3a Inhibitor 98.89%
    Nutlin-3a (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas[1][2].
  • HY-50696
    Nutlin-3 Inhibitor 99.06%
    Nutlin-3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.
  • 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[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.[12][1].
  • HY-158174
    Cbl-b-IN-20 Inhibitor
    Cbl-b-IN-20 (Example 50) is a casitas proto-oncogene-B ( CPL-B ) inhibitor with IC50 <100 nM[1].
  • HY-18643
    TZ9 Inhibitor 99.45%
    TZ9 is a selective Rad6 inhibitor. TZ9 inhibits Rad6B-induced histone H2A ubiquitination, downregulates intracellular β-catenin, induces G2-M arrest and apoptosis, and inhibits the proliferation and migration of metastatic human breast cancer cells[1].
  • HY-N0068
    Solasodine Inhibitor
    Solasodine (Purapuridine) is a steroidal alkaloid that occurs in plants of the Solanaceae family. Solasodine has neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic and anti-inflammatory activities[1][2].
  • HY-18986
    SAR405838 Inhibitor
    SAR405838 (MI-77301), an analog of MI-773, is a highly potent and selective MDM2-p53 interaction inhibitor. SAR405838 binds to MDM2 with a Ki of 0.88 nM. SAR405838 induces apoptosis and has potent antitumor activity[1][2].
  • HY-148266
    UBA5-IN-1 Inhibitor
    UBA5-IN-1 (compound 8.5) is a selective UBA5 inhibitor with an IC50 value of 4.0 μM. UBA5-IN-1 inhibits cell proliferation of Sk-Luci6 cancer cells with high expression levels of UBA5[1].
  • HY-16661
    Skp2 Inhibitor C1 Inhibitor 98.21%
    Skp2 Inhibitor C1 (SKPin C1) is an S-phase kinase-related protein 2 (Skp2) inhibitor with an inhibitory effect on metastatic melanoma cells. Skp2 Inhibitor C1 slows the cell cycle, inhibits cell proliferation, and triggers apoptosis[1].
  • HY-120934
    C25-140 99.86%
    C25-140, a first-in-class, orally active, and fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity[1].
  • HY-15335
    Nutlin-3b Inhibitor
    Nutlin-3b is a p53/MDM2 inhibitor with an IC50 of 13.6 μM. Nutlin-3b is 150 times less potent in binding to MDM2 than Nutlin-3a[1].
  • HY-N2360
    Hinokiflavone Inhibitor
    Hinokiflavone is a novel modulator of pre-mRNA splicing activity in vitro and in cellulo. Hinokiflavone blocks splicing of pre-mRNA substrates by inhibiting spliceosome assembly, specifically preventing B complex formation. Hinokiflavone is a SUMO protease inhibitor, inhibiting sentrin-specific protease 1 (SENP1) activity[1].
  • 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[1].
  • 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[1].
  • HY-126075
    WS-383 free base Inhibitor
    WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2[1].
  • HY-123967
    RNF5 inhibitor inh-02
    RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 leads to significant F508del-CFTR rescue (EC50=2.2 uM) in bronchial epithelial cells homozygous for the F508del mutation. RNF5 inhibitor inh-02 can be used for cystic fibrosis research[1].