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-148130A
    Rugonersen sodium
    Rugonersen sodium is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) sodium is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch.
    Rugonersen sodium
  • HY-134596
    SENP1-IN-3
    		Inhibitor 99.92%
    SENP1-IN-3 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 17. SENP1-IN-3 is developed for tumor radiosensitivity enhancement.
    SENP1-IN-3
  • HY-70027A
    p53 and MDM2 proteins-interaction-inhibitor dihydrochloride
    		Inhibitor 99.56%
    p53 and MDM2 proteins-interaction-inhibitor dihydrochloride is an inhibitor of the interaction between p53 and MDM2 proteins.
    p53 and MDM2 proteins-interaction-inhibitor dihydrochloride
  • HY-12287
    YH239-EE
    		Inhibitor 98.28%
    YH239-EE, ethyl ester of the free carboxylic acid compound YH239, is a potent p53-MDM2 antagonizing and apoptosis-inducing agent.
    YH239-EE
  • HY-148130
    Rugonersen
    		Activator
    Rugonersen (RG6091; RO7248824) is a locked-nucleic acid (LNA)- modified antisense oligonucleotides (ASOs), and results in reduction of ubiquitin-protein ligase E3A (UBE3A) silencing. Angelman syndrome (AS) is a severe neurodevelopmental disorder caused by the loss of neuronal E3 ligase UBE3A, Rugonersen has been used for AS reasearch.
    Rugonersen
  • HY-151799
    P62-RNF168 agonist-1
    		Agonist 98.62%
    P62-RNF168 agonist-1 (compound 5a) is a low cytotoxicity P62-RNF168 agonist that enhances the interaction between P62 and RNF168. P62-RNF168 agonist-1 induces a reduction in H2A ubiquitination mediated by RNF168 and impairs homologous recombination-mediated DNA repair. P62-RNF168 agonist-1 also inhibits the growth of xenograft tumors in mice in a dose-dependent manner.
    P62-RNF168 agonist-1
  • 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-161470
    WS-384
    		Inhibitor
    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-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-W264347
    DCN1-UBC12-IN-4
    		Inhibitor
    DCN1-UBC12-IN-4 (compound 5p) is an inhibitor of DCN1-UBC12, with an IC50 greater than 10000 nM, and it exhibits anti-tumor activity.
    DCN1-UBC12-IN-4
  • 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-160928
    Smurf1 modulator-1
    		Inhibitor 99.76%
    Smurf1 modulator-1 (Compound 20) is a selective inhibitor for Smad ubiquitination regulatory factor 1 (Smurf1), with IC50 of 180 nM.
    Smurf1 modulator-1
  • 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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity