1. Signaling Pathways
  2. Metabolic Enzyme/Protease
  3. 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

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-W340313
    p53-MDM2-IN-4
    Inhibitor 99.79%
    p53-MDM2-IN-4 (Example 4) is an inhibitor of p53-MDM2/X protein interaction, with a Ki value of 3.079 μM. p53-MDM2-IN-4 can be used in anti-tumor research.
    p53-MDM2-IN-4
  • HY-15954B
    NVP-CGM097 sulfate
    Inhibitor 98.82%
    NVP-CGM097 sulfate is a potent and selective MDM2 inhibitor with IC50 of 1.7±0.1 nM for hMDM2.
    NVP-CGM097 sulfate
  • HY-141482
    WSB1 Degrader 1
    Inhibitor 99.81%
    WSB1 Degrader 1 is a poten and orally active WSB1 (WD repeat and SOCS box-containing 1) degrader. WSB1 Degrader 1 has anticancer metastatic effects.
    WSB1 Degrader 1
  • HY-125858A
    MI-1061 TFA
    Inhibitor
    MI-1061 TFA is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 TFA potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
    MI-1061 TFA
  • HY-156768
    Cbl-b-IN-12
    Inhibitor
    Cbl-b-IN-12 (Example 10) is a casitas B-lineage lymphoma-b (CBL-B) inhibitor with an IC50 of <100 nM.
    Cbl-b-IN-12
  • HY-156382
    SPOP-IN-1
    Inhibitor 99.71%
    SPOP-IN-1 is a selective SPOP E3 ubiquitin ligase inhibitor. SPOP-IN-1 leads to the accumulation of tumor suppressors PTEN and DUSP7 and decreased levels of phosphorylated AKT and ERK in clear-cell renal cell carcinoma.
    SPOP-IN-1
  • HY-109045A
    Teslexivir hydrochloride
    Inhibitor 99.34%
    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.
    Teslexivir hydrochloride
  • HY-161470
    WS-384
    Inhibitor 98.23%
    WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC).
    WS-384
  • HY-134597
    SENP1-IN-4
    Inhibitor ≥98.0%
    SENP1-IN-4 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 21. SENP1-IN-4 is developed for tumor radiosensitivity enhancement.
    SENP1-IN-4
  • HY-W340839
    p53-MDM2-IN-1
    Inhibitor 99.91%
    p53-MDM2-IN-1 (Example 30) is an inhibitor of p53-MDM2/X protein interaction with an Ki value of 23.35 µM. p53-MDM2-IN-1 can be used for anti-tumor research.
    p53-MDM2-IN-1
  • HY-P3709
    TRAF6 peptide
    Inhibitor
    TRAF6 peptide is a specific TRAF6-p62 inhibitor. TRAF6 peptide potently abrogates NGF-dependent TrkA ubiquitination. TRAF6 peptide has good research potential in neurological diseases such as alzheimer's disease (AD), parkinson's, ALS, head trauma, epilepsy and stroke.
    TRAF6 peptide
  • HY-109045
    Teslexivir
    Inhibitor
    Teslexivir (BTA074) is a potent antiviral agent. Teslexivir 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 can be used for condyloma research.
    Teslexivir
  • HY-70027
    p53 and MDM2 proteins-interaction-inhibitor (chiral)
    Inhibitor 98.13%
    p53 and MDM2 proteins-interaction-inhibitor (chiral) (Compound 32) is an inhibitor of the interaction between p53 and MDM2 proteins.
    p53 and MDM2 proteins-interaction-inhibitor (chiral)
  • 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.
    WS-383 free base
  • HY-100507A
    Avadomide hydrochloride
    Modulator
    Avadomide hydrochloride (CC 122 hydrochloride) is the hydrochloride form of Avadomide (HY-100507). Avadomide hydrochloride is an orally active cereblon modulator. Avadomide hydrochloride modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide hydrochloride exhibits potent antitumor and immunomodulatory activities.
    Avadomide hydrochloride
  • HY-169005
    Cbl-b-IN-27
    Inhibitor
    Cbl-b-IN-27 is a casitas B-lymphoma proto-oncogene-b (Cbl-b) inhibitor with an IC50 value of 7 nM. Cbl-b-IN-27 is promising for research of effector T cell function, T cell, natural killer (NK) cell and B cell activation regulation.
    Cbl-b-IN-27
  • 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-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-160876
    BC-1901S
    BC-1901S is a proteasome-independent NRF2 activator and stabilizer. BC-1901S binds to DCAF1 (E3 ligase subunit) and disrupts NRF2/DCAF1 interaction, and activates NRF2 by inhibiting NRF2 ubiquitination in a KEAP1-independent manner. BC-1901S shows anti-inflammatory effect in a murine model of LPS-induced acute lung injury.
    BC-1901S
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity