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-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-W062696
    BC-1382
    Inhibitor 99.53%
    BC-1382 is a potent ubiquitin E3 ligase HECTD2 inhibitor that specificly disrupts the HECTD2/PIAS1 interaction (IC50≈ 5 nM).Anti-inflammatory activity.
    BC-1382
  • HY-156766
    Cbl-b-IN-10
    Inhibitor
    Cbl-b-IN-10 (Compound 463) is a casitas B-lineage lymphoma-b (Cbl-b) and c-Cbl inhibitor with IC50s of 6.0 nM and 3.5 nM, respectively.
    Cbl-b-IN-10
  • HY-161977
    Cbl-b-IN-26
    Inhibitor
    Cbl-b-IN-26 (Example A1) is a Cbl-b inhibitor with a Kd of 34.6 nM . Cbl-b-IN-26 can be used in the study of chronic viral infections and cancer.
    Cbl-b-IN-26
  • HY-157728
    ML307
    Inhibitor 99.10%
    ML307 is a potent, sub-micromolar, first-in-class Ubc13 enzyme activity inhibitor with an IC50 of 781 nM. ML307 has the potential for immunomodulation and inflammation research.
    ML307
  • 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-156769
    Cbl-b-IN-13
    Inhibitor
    Cbl-b-IN-13 (Example 520) is a Cbl-b inhibitor with an IC50 of <100 nM. Cbl-b-IN-13 has the ability to activate T-cells.
    Cbl-b-IN-13
  • HY-122210
    T521
    Inhibitor 99.9%
    T521 is an inhibitor of E3 ligase. T521 can be used in cancer and metabolic disease related research.
    T521
  • 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-N0170R
    Indole-3-carbinol (Standard)
    Inhibitor
    Indole-3-carbinol (Standard) is the analytical standard of Indole-3-carbinol. This product is intended for research and analytical applications. Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).
    Indole-3-carbinol (Standard)
  • 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-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-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-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