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-134823
    MD-222
    		Inhibitor 99.81%
    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-123578
    NSC689857
    		Inhibitor 99.49%
    NSC689857 is a potent EGFR and SCFSKP2 inhibitor with an IC50 value of 36 μM for Skp2-Cks1. NSC689857 can inhibit p27 ubiquitylation (IC50=30 μM). NSC689857 has varied activity across cancer types, with more activity against leukemia cell lines than others.
    NSC689857
  • HY-W229874
    EN106
    		Inhibitor 99.92%
    EN106 is a potent inhibitor of FEMIB. EN106 is a cysteine-reactive covalent ligand. EN106 disrupts recognition of the key reductive stress substrate of FEM1B, FNIP1. EN106 reduces oxidative stress and rescues high glucose-induced impaired angiogenesis in HUVECs.
    EN106
  • HY-128842
    PROTAC MDM2 Degrader-3
    		Inhibitor
    PROTAC MDM2 Degrader-3 is a MDM2 degrader based on PROTAC technology. PROTAC MDM2 Degrader-3 composes of a potent MDM2 inhibitor, linker, and the MDM2 ligand for E3 ubiquitin ligase.
    PROTAC MDM2 Degrader-3
  • HY-149316
    Smurf1-IN-1
    		Inhibitor 99.47%
    Smurf1-IN-1 is an orally active and selective inhibitor of specific E3 ubiquitin protein ligase 1 (SMURF1) with an IC50 of 92 nM. Smurf1-IN-1 has significant efficacy in rats model of pulmonary hypertension.
    Smurf1-IN-1
  • HY-17493
    MI-773
    		Inhibitor 98.08%
    MI-773 is a potent MDM2-p53 protein‐protein interaction (PPI) inhibitor with high binding affinity against MDM2 (Kd=8.2 nM). MI-773 has antitumor activity.
    MI-773
  • HY-128841
    PROTAC MDM2 Degrader-2
    		Inhibitor
    PROTAC MDM2 Degrader-2 is an MDM2 PROTAC degrader. PROTAC MDM2 Degrader-2 can induce the self-ubiquitination and degradation of MDM2, thereby upregulating the level of p53 protein. PROTAC MDM2 Degrader-2 has anti-tumor activity and can be used in the study of cancer. (Blue: MDM2 ligand (HY-128836); Black: linker (HY-128833))
    PROTAC MDM2 Degrader-2
  • HY-153937
    Skp2 inhibitor 2
    		Inhibitor 99.88%
    Skp2 inhibitor 2 (compound 14ag) is an inhibitor of F-box protein S-phase kinase-associated protein 2 (Skp2), with an IC50 value of 570 nM (Skp2-Cks1). Skp2 is a part of cullin-RING ligases, which recruits and ubiquitinates substrates, involving in proteolytic and non-proteolytic process.
    Skp2 inhibitor 2
  • HY-16664
    SJ-172550
    		Inhibitor 99.95%
    SJ-172550 is a small molecule inhibitor of MDMX; competes for the wild type p53 peptide binding to MDMX with an EC50 of 5 μM.
    SJ-172550
  • HY-153775
    UC-764864
    		Inhibitor 99.85%
    UC-764864 is a UBE2N inhibitor. UC-764864 inhibits UBE2N enzymatic activity. UC-764864 has cytotoxic effects and inhibition of UBE2N-dependent signaling in leukemic cells. UC-764864 blocks ubiquitination of innate immune- and inflammatory-related substrates in human AML cell lines.
    UC-764864
  • HY-16999
    RO8994
    		Inhibitor 99.62%
    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-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-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-145733
    DI-1859
    		Inhibitor 99.62%
    DI-1859 is a potent, selective and covalent inhibitor of DCN1. DI-1859 inhibits neddylation of cullin 3 in cells at low nanomolar concentrations. DI-1859 induces a robust increase of NRF2 protein, a CRL3 substrate, in mouse liver and effectively protects mice from acetaminophen-induced liver damage.
    DI-1859
  • HY-15301
    CC0651
    		Inhibitor 99.03%
    CC0651 is an allosteric inhibitor of the human Cdc34 ubiquitin-conjugating enzyme. CC0651 potently (IC50=1.72 μM) inhibits the ubiquitination of p27Kip1, as confirmed by dose-response analysis.
    CC0651
  • HY-122615B
    SPOP-IN-6b dihydrochloride
    		Inhibitor 99.70%
    SPOP-IN-6b dihydrochloride is a potent speckle-type POZ protein (SPOP) inhibitor with an IC50 of 3.58 μM.
    SPOP-IN-6b dihydrochloride
  • 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-114304
    COH000
    		Inhibitor 98.0%
    COH000 is an allosteric, covalent and irreversible inhibitor of ubiquitin-like 1-activating enzyme (SUMO-activating enzyme) (E1), with an IC50 of 0.2 μM for SUMOylation in vitro.
    COH000
  • 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
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity