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-180654
    JWZ-8-103
    		Modulator
    JWZ-8-103 is an orally active PRLX-93936 (HY-119264) analog and TRIM21-targeting molecular glue. JWZ-8-103 increases the thermal stability of TRIM21. JWZ-8-103 promotes a robust and rapid interaction between TRIM21 and NUP98 (apparent EC50 = ∼20 μM for TRIM21 PRYSPRY and NUP98 APD). JWZ-8-103 has anti-cancer effects against pancreatic cancer.
    JWZ-8-103
  • HY-W342380
    SPI-05
    		Inhibitor
    SPI-05 (NSC 5067) is a non-competitive SUMO-specific proteases (SENP1/2) inhibitor (IC50=60 μM). SPI-05 is promising for research of cancers, such as prostate cancer and hypoxia-driven solid tumors with SENP1 overexpression.
    SPI-05
  • HY-180548
    MRC37
    		Inhibitor 98.90%
    MRC37 is a potent and selective small-molecule ligand of TRIM21 that binds the PRYSPRY domain of TRIM21. MRC37 inhibits the natural antiviral function of TRIM21 by preventing antibody neutralisation of adenovirus 5 (Adv5). MRC37 is also capable of inhibiting Trim-Away, a targeted protein degradation technology where TRIM21 is recruited to specific proteins via electroporated antibodies.
    MRC37
  • HY-161901
    BC-1293
    		Inhibitor 98.40%
    BC-1293 is an inhibitor for E3 ligase subunit FBXO24. BC-1293 disrupts the interaction between FBXO24 and aspartyl-tRNA synthetase (DARS2) and increases the level of DARS2. BC-1293 increases levels of IL-1β, IL-9, MIP-2, and TNF α, and exhibits immunostimulatory activity in mice.
    BC-1293
  • HY-181653
    PROTAC SKP2 Degrader-1
    		Degrader
    PROTAC SKP2 Degrader-1 is a PROTAC degrader targeting SKP2, with a Kd value of 6.28 μM. PROTAC SKP2 Degrader-1 induces targeted degradation of SKP2 via the ubiquitin-proteasome system. PROTAC SKP2 Degrader-1 stabilizes the expression of SOCS1 and regulates the expression of immunoproteasomes through the JAK/STAT pathway, thereby inhibiting tumor cell proliferation. PROTAC SKP2 Degrader-1 is applicable for cancer-related research.
    PROTAC SKP2 Degrader-1
  • HY-N0068R
    Solasodine (Standard)
    		Inhibitor
    Solasodine (Standard) is the analytical standard of Solasodine. This product is intended for research and analytical applications. Solasodine (Purapuridine) is a steroidal alkaloid that occurs in plants of the Solanaceae family. Solasodine has neuroprotective, antifungal, hypotensive, anticancer, antiatherosclerotic, antiandrogenic and anti-inflammatory activities.
    Solasodine (Standard)
  • HY-161470
    WS-384
    		Inhibitor 98.23%
    WS-384 is a dual LSD1 and DCN1-UBC12 protein-protein interaction inhibitor with oral activity, with IC50 values of 338.79 nM and 14.81 nM, respectively. WS-384 possesses anticancer activity and can cause cell cycle arrest, DNA damage, and induce apoptosis. WS-384 can be used in the research of non-small cell lung cancer (NSCLC).
    WS-384
  • HY-174416
    Smurf1-IN-5
    		Inhibitor
    Smurf1-IN-5 (Compound cpd-6) is an allosteric SMAD ubiquitin regulatory factor 1 (SMURF1) inhibitor. Smurf1-IN-5 leads to a reduction in the ubiquitylation of substrates such as BMPR2 (bone morphogenetic protein receptor 2) and SMAD1, enhancing the BMP (bone morphogenetic protein) signaling pathway. Smurf1-IN-5 is promising for research of pulmonary arterial hypertension (PAH).
    Smurf1-IN-5
  • HY-157728
    ML307
    		Inhibitor 99.10%
    ML307 is a potent, sub-micromolar, first-in-class Ubc13 enzyme activity inhibitor with an IC50 of 781 nM. ML307 has the potential for immunomodulation and inflammation research.
    ML307
  • HY-180107
    H36-E4
    		Inhibitor 98.57%
    H36-E4 is a WW domain containing E3 ubiquitin 27 protein ligase 2 (WWP2) inhibitor with a KD of 6.25 μM. H36-E4 inhibits WWP2 expression, restores the succinate dehydrogenase complex subunit C (SDHC) level, and defers the acute kidney injury (AKI)-to-chronic kidney disease (CKD) transition in unilateral kidney ischemia-reperfusion (UIR) mice. H36-E4 can be used for AKI-to-CKD transition research.
    H36-E4
  • HY-134597
    SENP1-IN-4
    		Inhibitor 98.0%
    SENP1-IN-4 is a specific deSUMOylation protease 1 (SENP1) inhibitor extracted from patent CN110627860, Compound 21. SENP1-IN-4 is developed for tumor radiosensitivity enhancement.
    SENP1-IN-4
  • HY-122210
    T521
    		Inhibitor 99.73%
    T521 is an inhibitor of E3 ligase. T521 can be used in cancer and metabolic disease related research.
    T521
  • HY-P3709
    TRAF6 peptide
    		Inhibitor
    TRAF6 peptide is a specific TRAF6-p62 inhibitor. TRAF6 peptide potently abrogates NGF-dependent TrkA ubiquitination. TRAF6 peptide has good research potential in neurological diseases such as alzheimer's disease (AD), parkinson's, ALS, head trauma, epilepsy and stroke.
    TRAF6 peptide
  • HY-109045
    Teslexivir
    		Inhibitor
    Teslexivir (BTA074) is a potent antiviral agent. Teslexivir is a potent and selective inhibitor of the interaction between two essential viral proteins, E1 and E2, an association that is a necessary step in the DNA replication and thus viral production for Human Papilloma Virus (HPV) 6 and 11. Teslexivir can be used for condyloma research.
    Teslexivir
  • HY-70027
    p53 and MDM2 proteins-interaction-inhibitor (chiral)
    		Inhibitor 98.13%
    p53 and MDM2 proteins-interaction-inhibitor (chiral) (Compound 32) is an inhibitor of the interaction between p53 and MDM2 proteins.
    p53 and MDM2 proteins-interaction-inhibitor (chiral)
  • HY-12287
    YH239-EE
    		Inhibitor 98.28%
    YH239-EE, ethyl ester of the free carboxylic acid compound YH239, is a potent p53-MDM2 antagonizing and apoptosis-inducing agent.
    YH239-EE
  • HY-126075
    WS-383 free base
    		Inhibitor
    WS-383 free base is a potent, selective and reversible inhibitor of DCN1-UBC12 interaction, with an IC50 of 11 nM. WS-383 free base inhibits Cul3/1 neddylation, induces accumulation of p21, p27 and NRF2.
    WS-383 free base
  • HY-100507A
    Avadomide hydrochloride
    		Modulator
    Avadomide hydrochloride (CC 122 hydrochloride) is the hydrochloride form of Avadomide (HY-100507). Avadomide hydrochloride is an orally active cereblon modulator. Avadomide hydrochloride modulates cereblon E3 ligase activity, inhibits NF-κB pathway, arrests the cell cycle at G1 phase, and thus induces apoptosis in cancer cell PDAC. Avadomide hydrochloride exhibits potent antitumor and immunomodulatory activities.
    Avadomide hydrochloride
  • HY-169005
    Cbl-b-IN-27
    		Inhibitor
    Cbl-b-IN-27 is a casitas B-lymphoma proto-oncogene-b (Cbl-b) inhibitor with an IC50 value of 7 nM. Cbl-b-IN-27 is promising for research of effector T cell function, T cell, natural killer (NK) cell and B cell activation regulation.
    Cbl-b-IN-27
  • HY-D2259
    PFI-7
    PFI-7 is a probe, which binds to human GID4 (KD is 79 nM), and antagonizes the binding of Pro/N-degrons. PFI-7 can be utilized in C-terminal to LisH (CTLH) complex research and development of targeted protein degradation.
    PFI-7
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity