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-W176629
    Hydrocotarnine
    		Inhibitor 99.59%
    Hydrocotarnine is a Cbl inhibitor, and results in inflammasome-mediated IL-18 secretion in colitis. Hydrocotarnine increases expression of GLUT1 and cellular glucose uptake in glycolytic metabolism. Hydrocotarnine acts as an agent that provides analgesic effect in cancer research.
    Hydrocotarnine
  • HY-120086
    RO-5963
    		Inhibitor 98.19%
    RO-5963 is a dual p53-MDM2 and p53-MDMX inhibitor with IC50s of ~17 nM and ~24 nM, respectively.
    RO-5963
  • HY-158239
    MS181
    		Inhibitor 98.36%
    MS181 (compound 1) is a potent cereblon (CRBN)-recruiting and EED-binding polycomb repressive complex 1 (PRC1) PROTAC degrader. MS181 decreases the expression of EED, EZH2, SUZ12, BMI1 and RING1B. MS181 shows antiproliferative activity (Strtucture Note: Red, EED binder (HY-158771); Blue, CRBN ligand (HY-41547); Black, Linker HY-131717).
    MS181
  • HY-100383
    BH3I-1
    		Inhibitor ≥98.0%
    BH3I-1 is a Bcl-2 family antagonist, which inhibits the binding of the Bak BH3 peptide to Bcl-xL with a Ki of 2.4±0.2 μM in FP assay. BH3I-1 has a Kd of 5.3 μM against the p53/MDM2 pair.
    BH3I-1
  • HY-101266B
    Milademetan tosylate hydrate
    		Inhibitor 98.89%
    Milademetan (DS-3032) tosylate hydrate is a specific and orally active MDM2 inhibitor for the research of acute myeloid leukemia (AML) or solid tumors. Milademetan (DS-3032) tosylate hydrate induces G1 cell cycle arrest, senescence and apoptosis.
    Milademetan tosylate hydrate
  • HY-156395
    MN551
    		Inducer 98.05%
    MN551 is a potent inhibitor of cysteine-directed electrophilic covalent that plays important roles in the biology of SOCS2 and its CRL5 complex, and as E3 ligase handles in proteolysis targeting chimera (PROTACs) to induce targeted protein degradation.
    MN551
  • HY-161251
    SPOP-IN-2
    SPOP-IN-2 (compound E1) is a Speckle-type POZ protein (SPOP) inhibitor with IC50 of 0.58 μM, which disrupt the SPOP-subtrate interaction and selectively inhibits proliferation of ccRCC.
    SPOP-IN-2
  • HY-157416
    COP1-ATGL modulator 1
    		99.31%
    COP1-ATGL modulator 1 (86) is an orally active modulator for COP1-ATGL axis. COP1-ATGL modulator 1 (86) could increase ATGL protein expression, reduce ATGL ubiquitination and COP1 autoubiquitination, and diminish lipid accumulation in hepatocytes in the nanomolar range.
    COP1-ATGL modulator 1
  • HY-141448
    NRX-2663
    		Inhibitor 98.20%
    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-W184800
    MuRF1-IN-2
    		Inhibitor 99.05%
    MuRF1-IN-2 (Example 3) is a MuRF1 inhibitor. MuRF1-IN-2 can be used for research of muscle wasting conditions, of skeletal or cardial muscle atrophy.
    MuRF1-IN-2
  • HY-170430
    HGC652
    		Ligand 98.86%
    HGC652 is the molecular glue, that targets E3 ubiquitin ligase TRIM21, promotes the formation of a ternary complex between TRIM21 and NUP98, induces degradation of NUP155 and nuclear pore complex proteins, thereby causing the cell death. HGC652 inhibits the proliferation of multi cancer cells, according to the expression level of TRIM21.
    HGC652
  • HY-103046
    UbcH5c-IN-1
    		Inhibitor 99.84%
    UbcH5c-IN-1 (compound 6d) is a potent and selective small-molecule inhibitor of Ubiquitin-conjugating enzyme UbcH5c, with a Kd of 283 nM for E2 UbcH5c-IN-1 by covalent binding with Cys85. A promising lead compound for the development of new antirheumatoid arthritis (RA) agent.
    UbcH5c-IN-1
  • HY-162938
    Skp2 inhibitor 3
    		Inhibitor 98.07%
    Skp2 inhibitor 3 (E35), an antitumor agent, is a potent S‑Phase Kinase-associated Protein 2 (SKP2) inhibitor, with an IC50 of 4.86 μM for Skp2-Cks1 binding. Skp2 inhibitor 3 (E35) significantly inhibits colony formation and migration, as well as arrests the cell cycle at the S-phase.
    Skp2 inhibitor 3
  • HY-169329
    BIO-2007817
    		Modulator 99.35%
    BIO-2007817 is a Parkin positive allosteric modulators (PAMs). BIO-2007817 enhances the activity of wildtype Parkin. BIO-2007817 stimulates Parkin (an E3 ligase)autoubiquitination and induces the appearance of monoubiquitinated forms of Miro1 (EC50: 0.17 μM).
    BIO-2007817
  • HY-U00442
    CTX1
    		Inhibitor 98.50%
    CTX1 is a p53 activator that overcomes HdmX-mediated p53 repression. CTX1 exhibits potent anti-cancer activity in a mouse acute myeloid leukemia (AML) model system.
    CTX1
  • 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-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-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-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-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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity