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-148266
    UBA5-IN-1
    		Inhibitor 98.0%
    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.
    UBA5-IN-1
  • HY-15335
    Nutlin-3b
    		Inhibitor 98.78%
    Nutlin-3b, the inactive form of Nutlin-3 (HY-50696), 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 (HY-10029). Nutlin-3b is promising for research of cancers.
    Nutlin-3b
  • HY-N10159
    1-Benzyl-I3C
    		Inhibitor 99.68%
    1-Benzyl-I3C is a NEDD4-1 inhibitor with significant anticancer activity. 1-Benzyl-I3C can directly inhibit the ubiquitination activity of NEDD4-1 with an IC50 of 12.3μM, which is significantly better than its precursor compound I3C of 284μM. 1-Benzyl-I3C and its analogs showed good effects in inhibiting the proliferation of human melanoma cells, which is roughly related to their potency as NEDD4-1 enzyme inhibitors. By combining in vitro ubiquitination experiments and thermal stability analysis, 1-Benzyl-I3C was shown to be able to bind to the catalytic HECT domain of NEDD4-1.
    1-Benzyl-I3C
  • HY-18986
    SAR405838
    		Inhibitor 98.84%
    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.
    SAR405838
  • HY-100892
    MX69
    		Inhibitor 99.59%
    MX69 is an inhibitor of MDM2/XIAP, used for cancer treatment.
    MX69
  • HY-136262
    CRBN-6-5-5-VHL
    		Degrader 99.45%
    CRBN-6-5-5-VHL is a potent and selective von Hippel-Lindau-based cereblon (CRBN) degrader with a DC50 value of 1.5 nM. CRBN-6-5-5-VHL has almost no effect on the degradation of the neo-substrates IKZF1 and IKZF3. (Pink: VHL ligand (HY-125845); Blue: E3 Ligase ligand (HY-10984); Black: linker (HY-403544)).
    CRBN-6-5-5-VHL
  • HY-111760
    NRX-252262
    		99.57%
    NRX-252262 is a potent enhancer of the interaction between β-Catenin, and its cognate E3 ligase, SCFβ-TrCP, induces mutant β-catenin degradation, with an EC50 of 3.8 nM.
    NRX-252262
  • HY-103435
    Vialinin A
    		Inhibitor 99.90%
    Vialinin A (Terrestrin A) is a p-terphenyl compound that can be derived from a Chinese edible mushroom. Vialinin A is an inhibitor of ubiquitin-specific peptidase 4 (USP4) and has anti-inflammatory and antioxidant properties. Vialinin A can alleviate cerebral ischaemia-reperfusion injury-induced neurological deficits and neuronal apoptosis. Vialinin A promotes activation of Keap1-Nrf2-ARE signaling pathway and increases the protein degradation of Keap1. Vialinin A possesses various pharmacological activities in cancer, Kawasaki disease, asthma, and pathological scarring. Vialinin A is a potent inhibitor of TNF-α, USP4, USP5, and sentrin/SUMO-specific protease 1 (SENP1). Vialinin A can be studied in reseach for autoimmune diseases, cancer and ischaemic stroke.
    Vialinin A
  • HY-133558
    VII-31
    		Activator 99.63%
    VII-31 is a potent NEDDylation pathway activator to inhibit the tumor progression in vitro and in vivo. VII-31 induces apoptosis via intrinsic and extrinsic pathways.
    VII-31
  • HY-15301
    CC0651
    		Inhibitor 98.83%
    CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27Kip1, as confirmed by dose-response analysis.
    CC0651
  • HY-148900
    SCFSkp2-IN-2
    		Inhibitor 99.01%
    SCFSkp2-IN-2 (Compound AAA-237) is a Skp2 inhibitor with a KD of 28.77 μM. AAA-237 induces apoptosis of NSCLC cells and shows antitumor activities.
    SCFSkp2-IN-2
  • HY-13297
    PYZD-4409
    		Inhibitor 98.0%
    PYZD-4409 is a specific inhibitor of the ubiquitin-activating enzyme UBA1 with an IC50 of 20 μM (cell-free enzymatic assay). PYZD-4409 induces cell death in malignant cells and preferentially inhibits the clonogenic growth of primary acute myeloid leukemia cells.
    PYZD-4409
  • HY-W229874
    EN106
    		Inhibitor 99.92%
    EN106 is a potent inhibitor of FEMIB. EN106 is a cysteine-reactive covalent ligand. EN106 disrupts recognition of the key reductive stress substrate of FEM1B, FNIP1. EN106 reduces oxidative stress and rescues high glucose-induced impaired angiogenesis in HUVECs.
    EN106
  • HY-15954
    NVP-CGM097
    		Inhibitor 99.80%
    NVP-CGM097 is a potent and selective MDM2 inhibitor with IC50 of 1.7±0.1 nM for hMDM2.
    NVP-CGM097
  • HY-15694
    SMIP004
    		Inhibitor 99.79%
    SMIP004 is a SKP2 E3 ligase inhibitor, which downregulates SKP2 and to stabilise p27. SMIP004 is a cancer cell selective apoptosis inducer of human prostate cancer cells.
    SMIP004
  • HY-139662
    HB007
    		Inhibitor 99.73%
    HB007 is a small ubiquitin-related modifier 1 (SUMO1) degrader. HB007 induces ubiquitination and degradation of SUMO1, resulting in reduced tumor growth in vivo. HB007 can be used for the research of brain, breast, colon, and lung cancers.
    HB007
  • HY-111505
    NAcM-OPT
    		Inhibitor 98.69%
    NAcM-OPT is an orally bioavailable cullin neddylation 1 (DCN1) inhibitor, which potently inhibits the DCN1-UBE2M interaction.
    NAcM-OPT
  • HY-145733
    DI-1859
    		Inhibitor 99.62%
    DI-1859 is a potent, selective and covalent inhibitor of DCN1. DI-1859 inhibits neddylation of cullin 3 in cells at low nanomolar concentrations. DI-1859 induces a robust increase of NRF2 protein, a CRL3 substrate, in mouse liver and effectively protects mice from acetaminophen-induced liver damage.
    DI-1859
  • HY-148602
    KH-4-43
    		Inhibitor 99.72%
    KH-4-43 is an inhibitor of E3 CRL4. KH-4-43 inhibits E3 CRL4's core ligase complex and exhibits anticancer activity. KH-4-43 has a binding Kd to E3 ROC1-CUL4A CTD or the highly related ROC1-CUL1 CTD at 83 nM or 9.4 μM, respectively.
    KH-4-43
  • HY-49444
    EN450
    		98.59%
    EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism.
    EN450
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity