2. Signaling Pathways
  3. PROTAC
  4. Ligands for E3 Ligase

Ligands for E3 Ligase

E3 ligase-recruiting Moiety

Ligands for E3 Ligase

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A PROTAC (Proteolysis Targeting Chimeric Molecule) is a protein degrader comprised of a ligand for E3 ligase (E3 ligase binder), a linker and a ligand for target protein (target binder). The association between an E3 ligase and a target protein induced by a PROTAC will lead to the transfer of ubiquitin and degradation of the targeted protein.

E3 ligases catalyze the transfer of ubiquitin to targeted proteins and determine the specificity of the proteins. There are hundreds of E3 ligases in cells, but only a limited number of them are successfully used in reported PROTACs, such as VHL (von Hippel-Lindau disease tumor suppressor protein), CRBN (Cereblon), MDM2 (the mouse double minute 2 homologue) and IAP (inhibitor of apoptosis).

Ligands for E3 Ligase Isoform Specific Products:

Ligands for E3 Ligase Isoform Comparison
Cat. No. Product Name CAS No. Purity Chemical Structure
  • HY-149452
    SJ1008066 2758867-71-7
    SJ1008066 is a MAGE-A11 inhibitor with anIC50 of 0.13 μM. SJ 1008066 binds to the MAGE homology domain (MHD) and disrupts MAGE-A11:PCF11 interaction.
    SJ1008066
  • HY-144983
    E3 ligase Ligand 22 2377849-57-3
    E3 ligase Ligand 22 (compound 139) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway.
    E3 ligase Ligand 22
  • HY-173627
    (R,S,S)-VH032-Me 1948273-05-9
    (R,S,S)-VH032-Me is a ligand for E3 ubiquitin ligase. (R,S,S)-VH032-Me can be connected to the ligand for protein by a linker to form dTAGV-1-NEG (HY-145514A). PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
    (R,S,S)-VH032-Me
  • HY-169954
    CRBN ligand-10
    CRBN ligand-10 (compound 18) is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-10
  • HY-139541
    Pomalidomide-5-O-CH3 1547163-02-9
    Pomalidomide-5-O-CH3 is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-O-CH3 can be connected to the ligand for protein by a linker to form PROTAC.
    Pomalidomide-5-O-CH3
  • HY-174208
    KLHDC2-IN-1 1005275-19-3
    KLHDC2-IN-1 (Compound 6) is a ligand targeting the ubiquitin E3 ligase KLHDC2 (Kd: 160 nM). KLHDC2-IN-1 enables the synthesis of a PROTAC that can effectively degrade BRD4 in cells.
    KLHDC2-IN-1
  • HY-170861
    E3 ligase Ligand 58 1799506-32-3
    E3 ligase Ligand 58 is an E3 ligase ligand. E3 ligase Ligand 58 can be used for synthesis of PROTAC AH078 (HY-170859).
    E3 ligase Ligand 58
  • HY-181531
    IAP ligand 7
    IAP ligand 7 is an E3 ligase ligand. IAP ligand 7 can be conjugated with TEAD ligand (HY-181595) and linker (HY-181608) to synthesize PROTAC TEAD/IAP degrader-1 (HY-181594) .
    IAP ligand 7
  • HY-162411
    E3 ligase Ligand 24 3038773-47-3
    E3 ligase Ligand 24 (Compound 24) is a Potent Ligand for the E3 Ligase DCAF15 (IC50= 0.053 μM). Due to E3 ligase Ligand 24’s selectivity and potent binding characteristics, it is pivotal in the study of targeted protein degradation.
    E3 ligase Ligand 24
  • HY-128807
    E3 ligase Ligand 10 1073560-68-5
    E3 ligase Ligand 10 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 10 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
    E3 ligase Ligand 10
  • HY-147373
    DA-PROTAC 2488660-12-2
    DA-PROTAC is a potent PROTAC degrader of copper ion-transport proteins Atox1 and CCS. DA-PROTAC can bind both Atox1 and CCS proteins, and the complex can be bound to E3 ligase, leading to increased levels of ubiquitination of Atox1 and CCS and degradation of Atox1 and CCS proteins via the proteasome pathway. DA-PROTAC can be used for triple negative breast cancer research.
    DA-PROTAC
  • HY-128836
    (4R,5S)-Nutlin carboxylic acid 2306390-08-7
    (4R,5S)-Nutlin carboxylic acid is a MDM2 ligand and also a nutlin-3 derivative. (4R,5S)-Nutlin carboxylic acid can be linked to target protein ligands via a linker to form a PROTAC that can be used for targeting PARP1.
    (4R,5S)-Nutlin carboxylic acid
  • HY-158152
    PROTAC CRBN ligand-2
    PROTAC CRBN ligand-2 (12) is a Biguanide-PROTAC derivative, with an EC50 of 0.15 mM in KP4 cells. PROTAC CRBN ligand-2 (12) demonstrates the ability to alter levels of mitochondrial proteins, notably complexes I and IV.
    PROTAC CRBN ligand-2
  • HY-170371
    E3 ligase Ligand 47
    E3 ligase Ligand 47 is an E3 ligase ligand that can be used to synthesize PROTAC LDD39 (HY-159967).
    E3 ligase Ligand 47
  • HY-P5930
    HOXB7 8–25
    HOXB7 8–25 (MDM2 32-46) is an MDM2-derived peptide epitope and can elicit antigen-specifc and tumor-reactive CD4+ T cell responses.
    HOXB7 8–25
  • HY-128811
    E3 ligase Ligand 14 2241489-43-8
    E3 ligase Ligand 14 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 14 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
    E3 ligase Ligand 14
  • HY-170449
    E3 ligase Ligand 48
    E3 ligase Ligand 48 is a CRBN ligand for PROTAC AR Degrader-9 (HY-170448). PROTAC AR Degrader-9 (Compound c6) is a PROTAC degrader for androgen receptor, that degrades AR in human hair follicle papilla cells (HDPCs) with a DC50 of 262.38 nM.
    E3 ligase Ligand 48
  • HY-149307
    CYCA-117-70 1958262-04-8
    CYCA-117-70 is a DCAF1 ligand (KD: 70 μM). CYCA-117-70 is an ideal chemical handles for PROTACs recruiting DCAF1.
    CYCA-117-70
  • HY-180928
    LCK degrader-3 3095032-59-7
    LCK degrader-3 (Compound 20) is a CRBN-based LCK molecular glue degrader. LCK degrader-3 can be used in the research of acute lymphoblastic leukemia.
    LCK degrader-3
  • HY-W733885
    E3 ligase Ligand 38 2883704-45-6
    E3 ligase Ligand 38 serves as the E3 ligase ligand for PROTAC IRAK4 degrader-12 (HY-168586) and can be used in the synthesis of PROTACs.
    E3 ligase Ligand 38
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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