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-W453715
    Thalidomide-4-F,5-Br 2740657-28-5 99.37%
    Thalidomide-4-F,5-Br is a Thalidomide analogue. Thalidomide recruits E3 ligase for the ubiquitinylation and subsequent proteolysis of a target protein. This molecule may be derivatized through substitution at fluorine or bromine.
    Thalidomide-4-F,5-Br
  • HY-49514
    SOS1 Ligand intermediate-1 2380273-21-0
    VHL Ligand intermediate-1 (intermediate 18a) is an intermediate in the synthesis of VHL E3 ubiquitin ligase ligand and can be used to synthesize PROTACs.
    SOS1 Ligand intermediate-1
  • HY-W577257
    Thalidomide-1-Me,5-F 2230957-36-3
    5-Fluoro-2-(1-methyl-2,6-dioxo-3-piperidinyl)-1H-Isoindole-1,3(2H)-dione is a fluorinated E3 ligase activator. Thalidomide-1-Me,5-F may be used for further derivitization by SNAr.
    Thalidomide-1-Me,5-F
  • HY-149568
    Thalidomide-5-O-C11-NH2 hydrochloride
    Thalidomide-5-O-C11-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C11-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C11-NH2 hydrochloride
  • HY-W837135
    5-Hydrazinyl thalidomide hydrochloride 2803460-96-8
    5-Hydrazinyl thalidomide hydrochloride is a Thalidomide analogue featuring a hydrazine. PROTAC linkers are made to recruit E3 ligase for the ubiquitinylation of target proteins. The hydrazine may be used for further derivatization via reactions with various carbonyl groups.
    5-Hydrazinyl thalidomide hydrochloride
  • HY-W899002
    CRBN ligand-108 3036607-80-1
    CRBN ligand-108 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-108
  • HY-W834174
    Thalidomide-5-piperazine 2154342-61-5
    Thalidomide-5-piperazine is a Ligand for target protein for pROTAC.
    Thalidomide-5-piperazine
  • HY-149563
    Thalidomide-5-O-C6-NH2 hydrochloride 2761398-05-2
    Thalidomide-5-O-C6-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C6-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C6-NH2 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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