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-16999
    RO8994
    		Inhibitor 99.70%
    RO8994 (Compound 4) is an orally active, highly potent and selective spiroindolinone p53-MDM2 inhibitor with an IC50 value of 5 nM (HTRF binding assays) and 20 nM (MTT proliferation assays). RO8994 induces up-regulation of p53 expression and Apoptosis in wild-type p53 cancer cells. RO8994 also inhibits tumor growth in the tumor xenograft model.
    RO8994
  • HY-174346
    Skp2-IN-4
    		Inhibitor 98.60%
    Skp2-IN-4 is an Skp2 inhibitor with a IC50 of 0.38  μM for Skp2-Cks1 binding. Skp2-IN-4 improves anti-tumor activity, inhibits the proliferation and induces S phase arrest by targeting Skp2. Skp2-IN-4 significantly enhances Cisplatin (HY-17394) chemosensitivity by suppressing the tumor cell stemness in NCl-H1299 xenograft mice model, promising for lung cancer and esophageal cancer research.
    Skp2-IN-4
  • HY-129531
    MuRF1-IN-1
    		98.16%
    MuRF1-IN-1 is an orally active MuRF1 inhibitor. MuRF1-IN-1 can inhibit the interaction between MuRF1 and titin as well as E3 ligase activity. MuRF1-IN-1 can alleviate skeletal muscle atrophy and dysfunction in cardiac cachexia.
    MuRF1-IN-1
  • HY-155120
    Cbl-b-IN-5
    		Inhibitor 99.05%
    Cbl-b-IN-5 (compound 6) is a Cbl-b inhibitor (IC50=3-10 µM). Cbl-b-IN-5 has the potential to be used in the study of cancer and related diseases amenable to immune system modulation.
    Cbl-b-IN-5
  • HY-156373
    MN714
    		Inhibitor 99.12%
    MN714 is a pivaloyloxymethyl (POM) protected inhibitor.
    MN714
  • HY-141448
    NRX-2663
    		Inhibitor 98.96%
    NRX-2663 is an enhancer of the interaction between β-catenin, and its cognate E3 ligase, SCFβ-TrCP. NRX-2663 enhances the binding of β-catenin peptide for β-TrCP with an EC50 of 22.9 μM and a Kd of 54.8 nM.
    NRX-2663
  • HY-162683
    (S)-PHA533533
    		Modulator 98.27%
    (S)-PHA533533 is a CDK2 and CDK5 inhibitor with blood-brain barrier permeability, with IC50 values of 37 nM and 55 nM, respectively. (S)-PHA533533 effectively restores UBE3A expression by downregulating UBE3A-ATS and relieving the epigenetic silencing of paternal UBE3A in mature neurons. (S)-PHA533533 can be used for the research of Angelman syndrome.
    (S)-PHA533533
  • 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-160876
    BC-1901S
    		99.81%
    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-151799
    P62-RNF168 agonist-1
    		Agonist 98.03%
    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-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-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-103436
    NSC624206
    		Inhibitor 99.0%
    NSC624206 is an inhibitor of ubiquitin E1 (UBA1), with an IC50 of ~9 μM. NSC624206 specifically blocks ubiquitin-thioester formation (IC50=13 μM) but has no effect on ubiquitin adenylation.
    NSC624206
  • HY-151358
    SENP2-IN-1
    		Inhibitor 98.05%
    SENP2-IN-1 (compound 77) is a selective SENP2 inhibitor. SENP2-IN-1 shows inhibitory activities with IC50s of 1.3, 0.69 and 22.7 μM for SENP1, SENP2 and SENP5, respectively. SENP2-IN-1 can be used for the research of cancer.
    SENP2-IN-1
  • HY-155477
    Cbl-b-IN-15
    		Inhibitor 99.78%
    Cbl-b-IN-15 (compound 25) is an inhibitor of the RING finger E3 ligase Cbl (IC50: 15 nM). Cbl-b refers to Casitas B-lineage lymphoma proto-oncogene-b, which inhibits T-cell, natural killer (NK) cell, and B-cell activation. Cbl-b-IN-15 activates T cell function with EC50=0.41 μM.
    Cbl-b-IN-15
  • HY-170515
    RNF5 agonist 1
    		Agonist 99.05%
    RNF5 agonist 1 (analog-1), a structural analog of RNF5 inhibitor inh-02 (HY-123967), is a potent RNF5 agonist. RNF5 agonist 1 increases the ubiquitylation status of ATG4B in F508del-CFTR-expressing CFBE41o- cells.
    RNF5 agonist 1
  • HY-161977
    Cbl-b-IN-26
    		Inhibitor 99.81%
    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-173614
    CC-647
    		Modulator 99.58%
    CC-647 is a molecular glue modulator targeting Cereblon (CRBN) E3 ubiquitin ligase. CC-647 promotes the interaction between CRBN and ZBTB16 as well as its oncogenic fusion protein RARα-ZBTB16 (with a DC50 of 103 nM). CC-647 is promising for research of ZBTB16-RARα-associated acute promyelocytic leukemia (APL).
    CC-647
  • HY-180654A
    JWZ-8-103 hydrochloride
    		Modulator 99.93%
    JWZ-8-103 hydrochloride is an orally active PRLX-93936 (HY-119264) analog and TRIM21-targeting molecular glue. JWZ-8-103 hydrochloride increases the thermal stability of TRIM21. JWZ-8-103 hydrochloride promotes a robust and rapid interaction between TRIM21 and NUP98 (apparent EC50 = ∼20 μM for TRIM21 PRYSPRY and NUP98 APD). JWZ-8-103 hydrochloride has anti-cancer effects against pancreatic cancer.
    JWZ-8-103 hydrochloride
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Cat. No. Product Name / Synonyms Application Reactivity