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-160924
    MS147
    		98.31%
    MS147 is a VHL-based PROTAC degrader of BMI1 and RING1B (polycomb repressive complex 1 core components). MS147 directly binds EED and VHL E3 ligase, recruiting the ligase to the EED-BMI1/RING1B complex to induce time-dependent, ubiquitination-mediated degradation of BMI1 and RING1B. MS147 reduces histone H2A Lys119 mono-ubiquitination without altering histone H3 Lys27 tri-methylation and inhibits cancer cells proliferation. MS147 can be used for the research of cancer, such as chronic myelogenous leukemia and b-cell lymphoma. (Pink: BMI1/RING1B ligand (HY-183634); Blue: VHL ligand (HY-125845); Black: linker)
    MS147
  • 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-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-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-156395
    MN551
    		Inducer
    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-134594
    SENP1-IN-1
    		Inhibitor 99.55%
    SENP1-IN-1 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 29. SENP1-IN-1 is developed for tumor radiosensitivity enhancement.
    SENP1-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-134823
    MD-222
    		Inhibitor 98.03%
    MD-222 is the first-in-class highly potent PROTAC degrader of MDM2. MD-222 consists of ligands for Cereblon and MDM2. MD-222 induces rapid degradation of the MDM2 protein and activation of wild-type p53 in cells. MD-222 has anticancer effects.
    MD-222
  • HY-18643
    TZ9
    		Inhibitor 99.45%
    TZ9 is a selective Rad6 inhibitor. TZ9 inhibits Rad6B-induced histone H2A ubiquitination, downregulates intracellular β-catenin, induces G2-M arrest and apoptosis, and inhibits the proliferation and migration of metastatic human breast cancer cells.
    TZ9
  • 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-126075A
    WS-383
    		Inhibitor 99.43%
    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-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-153178
    HECT E3-IN-1
    		Inhibitor 99.44%
    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-170823
    PRC1-IN-1
    		Inhibitor
    PRC1-IN-1 is a PRC1 complex inhibitor. PRC1-IN-1 binds to both RING1A and RING1B proteins, and inhibits the activities of RING1B-BMI1 and RING1B-PCGF1. PRC1-IN-1 effectively inhibits H2AK119 ubiquitination and induces cell differentiation in leukemia cells. PRC1-IN-1 can be used for the research of leukemia.
    PRC1-IN-1
  • 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-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-W176629
    Hydrocotarnine
    		Inhibitor 99.70%
    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-W004883
    3-Amino-4,6-dimethylpyridine
    		Inhibitor 99.87%
    3-Amino-4,6-dimethylpyridine (5A-DMP) is a UHRF1 inhibitor that targets the Arg-binding cavity site within the UHRF1 TTD domain. 3-Amino-4,6-dimethylpyridine disrupts the interaction between UHRF1 and LIG1, interfering with DNA methylation, and can be utilized in cancer research.
    3-Amino-4,6-dimethylpyridine
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity