2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. E1/E2/E3 Enzyme
  5. E1/E2/E3 Enzyme Ligand

E1/E2/E3 Enzyme Ligand

E1/E2/E3 Enzyme Ligands (7):

Cat. No. Product Name Effect Purity
  • HY-181311
    CCT400028
    		Ligand 98.03%
    CCT400028 is a PROTACs-class degrader that targets the Aurora A (AURKA) kinase. CCT400028 induces ubiquitination and proteasomal degradation of target proteins by recruiting the cereblon (CRBN) E3 ubiquitin ligase. The KD values of CCT400028 against the three subtypes of human AURKA are 71 nM, 2100 nM and >10000 nM, respectively, and its IC50 against human CRBN is 6300 nM. CCT400028 is applicable to relevant research on leukemia, neuroblastoma and glioma.
  • HY-N0256
    Hederagenin
    		Ligand 99.95%
    Hederagenin is a triterpenoid saponin with orally active and antitumor activity. Hederagenin can inhibit the expression of iNOS, COX-2, and NF-κB in cells induced by LPS stimulation. Hederagenin also increases ROS production in cancer cells, disrupts mitochondrial membrane potential, and induces apoptosis. Hederagenin also sensitizes cancer cells to Cisplatin (HY-17394) and Paclitaxel (HY-B0015), enhancing induced apoptosis. Hederagenin can also bind to SKP2, with KD = 67.9 μM. Hederagenin also has preventive potential against alcoholic liver injury.
  • HY-170430
    HGC652
    		Ligand 98.86%
    HGC652 is a molecular glue degrader targeting TRIM21 with a TRIM21-dependent nuclear membrane disruption effect. HGC652 binds to the PRY-SPRY domain of TRIM21 with high affinity (Ka=0.061 μM), mediates the interaction between TRIM21 and NUP98, and redirects E3 ligase activity. By triggering the polyubiquitination and proteasomal degradation of nucleoporins (such as NUP155 and GLE1), HGC652 disrupts nuclear membrane integrity, alters nuclear morphology, induces genomic instability, and thereby induces cancer cell death.
  • HY-185652
    dTAG-TRIMTAC
    		Ligand
    dTAG-TRIMTAC is a PROTAC-like degrader targeting TRIM21. dTAG-TRIMTAC forms a ternary complex with TRIM21 and target proteins to drive degradation of oligomeric/assembled substrates via TRIM21 clustering-based activation, with degradation dependent on endogenous TRIM21. dTAG-TRIMTAC can be used for the research of neurodegenerative disease and inflammatory disease.
  • HY-P11481
    FITC-Acp-RpYTPEP-NH2
    		Ligand
    FITC-Acp-RpYTPEP-NH2 is a potent fluorescent tracer. FITC-Acp-RpYTPEP-NH2 shows a binding affinity (Kd = 0.07 μM) for the Cbl-b SH2 domain. Fluorescence polarization assay based on FITC-Acp-RpYTPEP-NH2 can be for evaluating Cbl-b SH2 domain inhibitors.
  • HY-174853
    TRIM25 ligand-1
    		Ligand
    TRIM25 ligand-1 (Compound 10) is a covalent ligand. TRIM25 ligand-1 can covalently bind to Cys498 in the PRYSPRY domain of TRIM25 and enhance its auto-ubiquitination activity. TRIM25 ligand-1 is selective for TRIM25 in vitro and in live cells.
  • HY-181287
    PROTAC CCR9 Degrader 1
    		Ligand
    PROTAC CCR9 Degrader 1 is a PROTAC-based degrader targeting CCR9. PROTAC CCR9 Degrader 1 induces ubiquitination, proteasomal degradation of CCR9 and reduces intracellular CCR9 levels by recruiting the VHL E3 ligase. PROTAC CCR9 Degrader 1 has a Ki value of 78.0 nM against human CCR9. PROTAC CCR9 Degrader 1 modulates GPCR activity by binding to the intracellular allosteric binding site of CCR9. PROTAC CCR9 Degrader 1 can be used in research related to Crohn's disease.