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-100487
    TAK-243
    		Inhibitor 98.38%
    TAK-243 (MLN7243) is a first-in-class, selective ubiquitin activating enzyme, UAE (UBA1) inhibitor (IC50=1 nM), which blocks ubiquitin conjugation, disrupting monoubiquitin signaling as well as global protein ubiquitination. TAK-243 (MLN7243) induces endoplasmic reticulum (ER) stress, abrogates NF-κB pathway activation and promotes apoptosis.
    TAK-243
  • HY-10029
    Nutlin-3a
    		Inhibitor 99.13%
    Nutlin-3a (Rebemadlin), an active enantiomer of Nutlin-3, is a potent murine double minute (MDM2) inhibitor (IC50=90 nM). Nutlin-3a inhibits MDM2-p53 interactions and stabilizes the p53 protein, and induces cell autophagy and apoptosis. Nutlin-3a has the potential for the study of TP53 wild-type ovarian carcinomas.
    Nutlin-3a
  • HY-111789
    Subasumstat
    		Inhibitor 98.53%
    Subasumstat (TAK-981) is a first in class and selective inhibitor of the SUMOylation enzymatic cascade, with potential immune-activating and antineoplastic activities.
    Subasumstat
  • HY-50696
    Nutlin-3
    		Inhibitor 99.18%
    Nutlin-3 is a commercial available p53-MDM2 inhibitor, with Ki of 90 nM.
    Nutlin-3
  • HY-15676
    Idasanutlin
    		Inhibitor 99.93%
    Idasanutlin (RG7388) is a potent and selective MDM2 antagonist, inhibiting p53-MDM2 binding, with an IC50 of 6 nM.
    Idasanutlin
  • HY-W1128879
    XMU-MP-8
    		Degrader 99.23%
    XMU-MP-8 (SKPer1) is a potent molecular glue degrader that targets the oncoprotein SKP2. XMU-MP-8 simultaneously binds to the F-box domain of SKP2 (Kd ≈ 36 μM) and the N-terminal TPR domain of the E3 ligase STUB1 (Kd ≈ 2.5 μM), forming a stable SKP2-SKPer1-STUB1 ternary complex (Kd ≈ 8.9 nM) that induces SKP2 ubiquitination and proteasomal degradation. XMU-MP-8 selectively eliminates SKP2-expressing cancer cells. XMU-MP-8 exhibits substantial tumour suppression with good safety profiles in vivo. XMU-MP-8 can be used for cancer research, such as non-small cell lung adenocarcinoma (NSCLC) and prostatic adenocarcinoma.
    XMU-MP-8
  • HY-174346
    Skp2-IN-4
    		Inhibitor
    Skp2-IN-4 is an Skp2 inhibitor with a IC50 of 0.38  μM for Skp2-Cks1 binding. Skp2-IN-4 improves anti-tumor activity, inhibits the proliferation and induces S phase arrest by targeting Skp2. Skp2-IN-4 significantly enhances Cisplatin (HY-17394) chemosensitivity by suppressing the tumor cell stemness in NCl-H1299 xenograft mice model, promising for lung cancer and esophageal cancer research.
    Skp2-IN-4
  • HY-173614
    CC-647
    		Modulator
    CC-647 is a molecular glue modulator targeting Cereblon (CRBN) E3 ubiquitin ligase. CC-647 promotes the interaction between CRBN and ZBTB16 as well as its oncogenic fusion protein RARα-ZBTB16 (with a DC50 of 103 nM). CC-647 is promising for research of ZBTB16-RARα-associated acute promyelocytic leukemia (APL).
    CC-647
  • HY-N0527
    Pentagalloylglucose
    		Inhibitor 99.77%
    Pentagalloylglucose (Penta-O-galloyl-β-D-glucose) is an orally active gallic tannin compound and an inducer of apoptosis and autophagy. Pentagalloglucose induces cell apoptosis and autophagy through the GSK3β/β-catenin pathway. Pentagalloylglucose inhibits UBE2T-mediated p53 ubiquitination, upregulates p53, downregulates RRM1/RRM2 in pancreatic cancer organoids. Pentagalloglucose has antioxidant, anti mutagenic, anti-inflammatory, anticonvulsant, cardioprotective, anti allergic, cholesterol lowering, and anti-tumor activities.
    Pentagalloylglucose
  • HY-129395
    Mezigdomide
    		Inhibitor 99.16%
    Mezigdomide (CC-92480), a cereblon E3 ubiquitin ligase modulating agent (CELMoD), acts as a molecular glue. Mezigdomide shows high affinity to cereblon, resulting in potent antimyeloma activity.
    Mezigdomide
  • HY-108702
    ML-792
    		Inhibitor 99.76%
    ML-792 is a potent and selective inhibitor of SAE/SUMO1 and SAE/SUMO2 in enzymatic assays (IC50 values of 3 and 11 nM, respectively) compared with NAE/NEDD8 and UAE/ubiquitin (IC50> values of 32 μM and >100 μM, respectively).
    ML-792
  • HY-114166
    2-D08
    		Inhibitor 99.17%
    2-D08 is a cell permeable, mechanistically unique inhibitor of protein SUMOylation. 2-D08 also inhibits Axl with an IC50 of 0.49 nM.
    2-D08
  • HY-12296
    Navtemadlin
    		Inhibitor 99.61%
    Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM.
    Navtemadlin
  • HY-13296
    PYR-41
    		Inhibitor 98.0%
    PYR-41 is a selective and cell permeable inhibitor of ubiquitin-activating enzyme E1 with an IC50 of < 10 μM, with little activity at E2 and E3.
    PYR-41
  • HY-120934
    C25-140
    		99.92%
    C25-140, a first-in-class, orally active, and fairly selective TRAF6-Ubc13 inhibitor, directly binds to TRAF6, and blocks the interaction of TRAF6 with Ubc13. C25-140 lowers TRAF6 activity, reduces NF-κB activation, and combats autoimmunity.
    C25-140
  • HY-N0170
    Indole-3-carbinol
    		Inhibitor 98.38%
    Indole-3-carbinol (I3C) inhibits NF-κB activity and also is an Aryl hydrocarbon receptor (AhR) agonist, and an inhibitor of WWP1 (WW domain-containing ubiquitin E3 ligase 1).
    Indole-3-carbinol
  • HY-110204
    Heclin
    		Inhibitor 98.21%
    Heclin is a HECT E3 ubiquitin ligases inhibitor. Heclin inhibits Smurf2, Nedd4, WWP1 (IC50 values are 6.8, 6.3, 6.9 μM) and can be used for the research of gastric cancer.
    Heclin
  • HY-139514
    RB-3
    		Inhibitor 99.42%
    RB-3, a polycomb repressive complex 1 (PRC1) inhibitor, binds to RING1B-BMI1f, with a Kd of 2.8 μM.
    RB-3
  • HY-122882
    HOIPIN-8
    		98.90%
    HOIPIN-8 is a potent inhibitor of linear ubiquitin chain assembly complex (LUBAC) with an IC50 of 11 nM. HOIPIN-8 is a HOIPIN-1 derivative with enhanced the potency by 255-fold in the petit-LUBAC inhibition, and 10-fold and 4-fold in the LUBAC- and TNF-α-mediated NF-κB activation, respectively than HOIPIN-1. HOIPIN-1 is a promising tool to explore the cellular functions of LUBAC.
    HOIPIN-8
  • HY-19817
    PRT4165
    		Inhibitor 98.0%
    PRT4165 is a potent inhibitor of polycomb-repressive complex 1 (PRC1)-mediated H2A ubiquitylation.
    PRT4165
Cat. No. Product Name / Synonyms Species Source
Cat. No. Product Name / Synonyms Application Reactivity