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-W077589A
    Lenalidomide-5-aminomethyl 1010100-28-3
    Lenalidomide-5-aminomethyl is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-5-aminomethyl can be connected to the ligand for protein by a linker to form PROTAC.
    Lenalidomide-5-aminomethyl
  • HY-161467
    Aster-A Ligand-3 2375541-28-7
    Aster-A Ligand-3 is a target protein ligand and can be used to synthesize PROTAC Aster-A degrader (HY-D2336).
    Aster-A Ligand-3
  • HY-161199
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C2-OH
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-pyrrolidine-C-piperidine-C2-OH can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C2-OH
  • HY-161639
    E3 ligase Ligand 26 2911613-35-7
    E3 ligase Ligand 26 (part of Compd 10) is a ligand for E3 ligase, used for the synthesis of PROTAC SOS1 degrader (HY-161636).
    E3 ligase Ligand 26
  • HY-128806
    E3 ligase Ligand 9 87304-15-2
    E3 ligase Ligand 9 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 9 can be connected to the ligand for protein by a linker to form PROTACs or SNIPERs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
    E3 ligase Ligand 9
  • HY-157560
    KDRLKZ-3
    KDRLKZ-3 is a selective E3 ligase. KDRLKZ-3 is a ligand for KLHDC2 with a IC50 value of 4.1 μM in the alphaLISA experiment.
    KDRLKZ-3
  • HY-170353
    E3 ligase Ligand 46 3033591-48-6
    E3 ligase Ligand 46 is a ligand for E3 ligase, used for the synthesis of PROTAC SMARCA2/4 degrader-36 (HY-170347).
    E3 ligase Ligand 46
  • HY-161210
    Thalidomide-azetidine-C-PIP-C-boc 2589699-87-4
    Thalidomide-azetidine-C-PIP-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-C-PIP-C-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-azetidine-C-PIP-C-boc
  • HY-161193
    Thalidomide-piperazine-(R)-C-pyrrolidine-C-boc
    Thalidomide-piperazine-(R)-C-pyrrolidine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperazine-(R)-C-pyrrolidine-C-boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-piperazine-(R)-C-pyrrolidine-C-boc
  • HY-161200
    Thalidomide-piperazine-C-azetidine-C2-OH
    Thalidomide-piperazine-C-azetidine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperazine-C-azetidine-C2-OH can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-piperazine-C-azetidine-C2-OH
  • HY-W1003189
    E3 ligase Ligand 42 2753651-18-0
    E3 ligase Ligand 42 is an E3 ubiquitin ligase ligand. E3 ligase Ligand 42 can be connected to the target protein ligand through a linker and can be used to synthesize PROTAC AR Degrader-6 (HY-156751). PROTAC can induce ubiquitination degradation of cancer-promoting proteins.
    E3 ligase Ligand 42
  • 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-173369
    PROTAC MAGL degrader-1
    PROTAC MAGL degrader-1 is an orally active PROTAC agent that simultaneously targets monoacylglycerol lipase (MAGL) and E3 ubiquitin ligase MDM2. PROTAC MAGL degrader-1 degrades MAGL and inhibits the binding of MDM2 to p53. PROTAC MAGL degrader-1 can partially penetrate the blood-brain barrier (BBB). PROTAC MAGL degrader-1 induces glioblastoma stem cells (GSCs) apoptosis. (E3 ligase ligand: HY-128837; target protein ligand + linker: HY-173370; target protein inhibitor: HY-15249).
    PROTAC MAGL degrader-1
  • 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 (MDM2 ligand 2) is the Nutlin 3-based MDM2 ligand. (4R,5S)-Nutlin carboxylic acid can be connected to the ligand for protein by a linker to form PROTACs.
    (4R,5S)-Nutlin carboxylic acid
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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