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-49444
    EN450
    		98.59%
    EN450 is a cysteine-reactive covalent molecular glue degrader targeting NF-κB. EN450 interacts with allosteric C111 in the E2 ubiquitin ligase UBE2D. EN450 induces the ternary complex formation between UBE2D and NFKB1. EN450 exerts its anti-proliferative effects through a Cullin E3 ligase and proteasome-dependent mechanism.
    EN450
  • HY-157435
    PELI1-IN-1
    		Inhibitor 98.02%
    PELI1-IN-1 (compound 3d) is a potent inhibitor of PELI1, E3 ubiquitin ligase. PELI1-IN-1 has anti-tumPELI1-IN-1, a Resveratrol (HY-16561) derivative, is an orally active PELI1 Inhibitor (Kd = 8.2 μM). PELI1-IN-1 markedly interrupts the interaction of PELI1 and SNAIL/SLUG, and inhibits the K63-polyubiquitization of SNAIL/SLUG by PELI1, subsequently downregulating the protein levels of epithelial-mesenchymal transition (EMT) effectors SNAIL/SLUG. PELI1-IN-1 significantly reduces the level of SNAIL, SLUG and Vimentin without affecting the PELI1 expression. PELI1-IN-1 targets the FHA domain of PELI1 and disrupts the interaction, leading to the anti-metastasis of TNBC cells in vitro and in vivo. PELI1-IN-1 shows no evident toxicity in vivo.
    PELI1-IN-1
  • HY-162938
    Skp2 inhibitor 3
    		Inhibitor 98.07%
    Skp2 inhibitor 3 is an orally active inhibitor of the Skp2-Cks1 complex, with an IC50 of 4.86 μM. Skp2 inhibitor 3 reduces Skp2 protein expression while upregulating the expression of p21 and p27. Skp2 inhibitor 3 inhibits colony formation and migration of cancer cells, and induces cell cycle arrest at the S phase. Skp2 inhibitor 3 suppresses tumor growth in xenograft mice. Skp2 inhibitor 3 can be used in the research of gastric cancer and prostate cancer.
    Skp2 inhibitor 3
  • HY-153937
    Skp2 inhibitor 2
    		Inhibitor 99.88%
    Skp2 inhibitor 2 is a Skp2-Cks1 protein-protein interaction inhibitor with a human IC50 of 0.57 μM. Skp2 inhibitor 2 binds to Skp2 at the interaction interface to block Skp2-Cks1 complex formation. Skp2 inhibitor 2 can be used for the research of gastric cancer, non-small cell lung cancer, breast cancer, prostate cancer.
    Skp2 inhibitor 2
  • HY-164027
    MyoMed 205
    		Inhibitor 99.31%
    MyoMed 205 is an orally active muscle ring finger protein 1 (MuRF1) inhibitor. MyoMed-205 reduces ubiquitination and subsequent proteasomal degradation of muscle proteins by inhibiting MuRF1 activity. MyoMed 205 augments muscle performance, attenuates muscle weight loss and alleviates disease-induced weight loss. MyoMed 205 can be used for the research of cancer cachexia, type 2 diabetes mellitus, and heart failure with preserved ejection fraction.
    MyoMed 205
  • 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-10949
    SMER3
    		Inhibitor 98.33%
    SMER3, a Rapamycin enhancer, is a selective Skp1-Cullin-F-box (SCF)Met30 ubiquitin ligase inhibitor. SMER3 enhances Rapamycin's growth inhibitory effect by inhibition of SCFMet30.
    SMER3
  • 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-125858
    MI-1061
    		Inhibitor 99.08%
    MI-1061 is a potent, orally bioavailable, and chemically stable MDM2 (MDM2-p53 interaction) inhibitor (IC50=4.4 nM; Ki=0.16 nM). MI-1061 potently activates p53 and induces apoptosis in the SJSA-1 xenograft tumor tissue in mice. Anti-tumor activity.
    MI-1061
  • 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-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-163638
    BRD4 degrader-1
    		99.85%
    BRD4 degrader-1 (Compound mL 1-50) is a relatively selective, monovalent and covalent BRD4 Molecular glue degrader. BRD4 degrader-1 induces degradation of both long and short isoforms of BRD4 by targeting DCAF16 (an E3 ligase). BRD4 degrader-1 can be used in breast cancer research.
    BRD4 degrader-1
  • HY-16664
    SJ-172550
    		Inhibitor 99.74%
    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 99.89%
    UC-764864 is a selective UBE2N inhibitor. UC-764864 covalently binds UBE2N catalytic Cys87, blocks ubiquitin-UBE2N thioester formation and polyubiquitin chain synthesis. UC-764864 blocks ubiquitination of innate immune- and inflammatory-related substrates, and induces cell apoptosis. UC-764864 can be used for the research of acute myeloid leukemia.
    UC-764864
  • 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-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-128845
    PROTAC CRBN Degrader-1
    		Degrader 98.77%
    PROTAC CRBN Degrader-1 (Compound 14a) is a VHL-CRBN heterodimerization PROTAC degrader that achieves a selective degradation of CRBN by binding two E3 ubiquitin ligases (VHL and CRBN) to each other. (Blue: VHL ligand (S,R,S)-AHPC (HY-125845); Pink: CRBN ligand Pomalidomide-C2-NH2 (HY-128846); Black: Linker (HY-128847))
    PROTAC CRBN Degrader-1
  • 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-123967
    RNF5 inhibitor inh-02
    		Inhibitor 99.91%
    RNF5 inhibitor inh-02 is a potent inhibitor of E3 ubiquitin ligase RNF5/RMA1. RNF5 inhibitor inh-02 rescues F508del-CFTR function in F508del-CFTR-expressing immortalized cells (CFBE41o⁻, EC50 = 2.6 μM; FRT, EC 50 = 2.2 μM). RNF5 inhibitor inh-02 increases LC3IIB expression and autophagic vacuole number via reducing ATG4B ubiquitylation and promotes cell motility. RNF5 inhibitor inh-02 can be used for the study of cystic fibrosis.
    RNF5 inhibitor inh-02
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity