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-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
  • HY-W584520
    Thalidomide-4-NH-PEG1-NH-Boc 2154342-17-1
    Thalidomide-4-NH-PEG1-NH-Boc is a Boc-modified Thalidomide (HY-14658) that acts as a Cereblon ligand to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-4-NH-PEG1-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-NH-PEG1-NH-Boc is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
    Thalidomide-4-NH-PEG1-NH-Boc
  • 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-163236
    Thalidomide-piperidine-O-azetidine-acetic acid
    Thalidomide-piperidine-O-azetidine-acetic acid is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperidine-O-azetidine-acetic acid can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-piperidine-O-azetidine-acetic acid
  • 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-157566
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride 2520105-60-4
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride is a functionalized cerebellar ligand for PROTAC development, combining E3 ligand and terminal piperidine for subsequent chemical reactions. A protein degradant with a rigid connector is generated.
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride
  • HY-156170
    Thalidomide-5-NH-PEG5-NH2 hydrochloride
    Thalidomide-5-NH-PEG5-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5-NH-PEG5-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-NH-PEG5-NH2 hydrochloride
  • HY-W584522
    Thalidomide-4-NH-PEG1-COO(t-Bu) 2140807-19-6
    Thalidomide-4-NH-PEG1-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-4-NH-PEG1-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-NH-PEG1-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
    Thalidomide-4-NH-PEG1-COO(t-Bu)
  • HY-161196
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C-boc
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-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-2,6-diazaspiro[3.4]octane-C-piperidine-C-boc
  • HY-160244
    Pomalidomide 5'-piperazine-4-methylpiperidine dihydrochloride 2758431-93-3
    Pomalidomide 5'-piperazine-4-methylpiperidine dihydrochloride is the Pomalidomide (HY-10984)-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide 5'-piperazine-4-methylpiperidine dihydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
    Pomalidomide 5'-piperazine-4-methylpiperidine dihydrochloride
  • HY-138678B
    (S,R,R)-VH032 2489876-59-5
    (S,R,R)-VH032 is a VHL ligand. (S,R,R)-VH032 can be used for synthesis of PROTAC NCOA4 degrader-1 (HY-163897).
    (S,R,R)-VH032
  • HY-157759
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-C2-OH
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-C2-OH can serve as a Cereblon ligand to recruit CRBN proteins and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-O-C2-OH
  • HY-150839
    E3 ligase Ligand PG 14149-34-9
    E3 ligase Ligand PG is a E3 ligase ligand that can be used in the recruitment of CRBN protein. E3 ligase Ligand PG exhibits potent binding activity with CRBN (IC50 of 2.191 μM). E3 ligase Ligand PG can be connected to the BMS-202 (HY-19745) by a linker to form PROTAC, PROTAC PD-L1 degrader-1 (HY-163757).
    E3 ligase Ligand PG
  • HY-163953
    (S,R,S)-AHPC-Ala 2641319-58-4
    (S,R,S)-AHPC-Ala is a ligand for E3 ubiquitinase. (S,R,S)-AHPC-Ala can be used to synthesize PROTAC SMARCA2/4-degrader-23 (HY-163876).
    (S,R,S)-AHPC-Ala
  • HY-W259932
    Lenalidomide 5'-piperazine 2222120-31-0 99.92%
    Lenalidomide 5'-piperazine is a functionalized cerebellar ligand for PROTAC development that binds an E3 ligand to terminal piperazine for subsequent chemical reactions to produce a protein deactivator with a rigid linker.
    Lenalidomide 5'-piperazine
  • HY-14658S
    Thalidomide-d4 1219177-18-0 98.03%
    Thalidomide-d4 is a deuterium labeled Thalidomide. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties[1][2].
    Thalidomide-d<sub>4</sub>
  • HY-157588
    (S)-Thalidomide-Piperazine-CH2-Pyrrolidine-C2-OH
    E3 ligase Ligand-Linker Conjugate 30 is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. E3 ligase Ligand-Linker Conjugate 30 can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (S)-Thalidomide-Piperazine-CH2-Pyrrolidine-C2-OH
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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