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

Related Products

PDF 1.36 MB

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-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-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-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-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-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-155120
    Cbl-b-IN-5
    		Inhibitor 99.61%
    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-126075A
    WS-383
    		Inhibitor 99.88%
    WS-383 is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
    WS-383
  • HY-163638
    BRD4 degrader-1
    		99.85%
    BRD4 degrader-1 (Compound ML 1-50) is a monovalent and covalent molecular glue BRD4 degrader. BRD4 degrader-1 targets DCAF16 (E3 ligase) and degrades both the long and short isoforms of BRD4 in cells.
    BRD4 degrader-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-153178
    HECT E3-IN-1
    		Inhibitor 99.43%
    HECT E3-IN-1 (compound 3) is a HECT E3 ligase inhibitor. HECT E3-IN-1 (compound 3) disrupts Ub binding to the noncovalent Ub-binding site of Nedd4-1.
    HECT E3-IN-1
  • 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-148130
    Rugonersen
    		Activator 98.50%
    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-160924
    MS147
    		Inhibitor 98.03%
    MS147 is a VHL-based PROTAC degrader of PRC1 (Polycomb Repressive Complex 1). The dissociation constants (Kd) of MS147 for EED (Embryonic Ectoderm Development) and VHL (Von Hippel-Lindau) are 3.0 μM and 450 nM, respectively. MS147 specifically binds to the EED protein through its EED-binding moiety; EED is a core component of PRC2 (Polycomb Repressive Complex 2) and interacts with the core components of PRC1, BMI1 (B-lymphoma Mo-MLV insertion region 1 homolog) and RING1B (Ring Finger Protein 1B). By this binding, MS147 is able to recruit BMI1 and RING1B near to VHL. Through the degradation of BMI1 and RING1B, MS147 reduces the level of H2AK119ub (histone H2A lysine 119 ubiquitination), affecting the proliferation of cancer cells. (Blue: VHL ligand (HY-125845), Black: linker ; Pink: PRC1 ligand (HY-158771)).
    MS147
  • 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-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-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-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-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-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