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-171775
    CRBN ligand-184 2259851-81-3
    CRBN ligand-184 is a ligand for CRBN-type E3 ubiquitin ligases. CRBN ligand-184 can be used to synthesize PROTAC AU-24118 (HY-163410).
    CRBN ligand-184
  • HY-156161
    Thalidomide-NH-C13-NH2 hydrochloride
    Thalidomide-NH-C13-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-NH-C13-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-NH-C13-NH2 hydrochloride
  • HY-W1111714
    3-(5-Bromo-2-chlorophenyl)piperidine-2,6-dione 2990057-63-9
    3-(5-Bromo-2-chlorophenyl)piperidine-2,6-dione is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    3-(5-Bromo-2-chlorophenyl)piperidine-2,6-dione
  • HY-W591352
    Thalidomide-5-(C6-amine) 1950635-17-2
    Thalidomide-5-(C6-amine) is a PROTAC building block that contains an E3 ligase ligand substituted with a terminal amine group. The amine group can react with NHS ester group or carboxylic acid in the presence of EDC or HATU.
    Thalidomide-5-(C6-amine)
  • HY-149567
    Thalidomide-5-O-C10-NH2 hydrochloride 99.37%
    Thalidomide-5-O-C10-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C10-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C10-NH2 hydrochloride
  • HY-W898998
    CRBN ligand-164 3036607-71-0
    CRBN ligand-164 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-164
  • HY-156171
    Thalidomide-5-NH-PEG6-NH2 hydrochloride
    Thalidomide-5-NH-PEG6-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-NH-PEG6-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-NH-PEG6-NH2 hydrochloride
  • HY-W899000
    CRBN ligand-162 3036607-75-4
    CRBN ligand-162 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-162
  • HY-W877989
    BWA-522 intermediate-1 2241315-66-0 99.27%
    BWA-522 intermediate-1 is an intermediate in the synthesis of PROTAC BWA-522 (HY-149433) and serves as a ligand molecule for cereblon E3 ubiquitin ligase. BWA-522 is an orally active small molecule protein-targeting chimera (PROTAC) that has significant degradation effects on AR-FL and AR-V7.
    BWA-522 intermediate-1
  • HY-149564
    Thalidomide-5-O-C7-NH2 hydrochloride 98.13%
    Thalidomide-5-O-C7-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C7-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C7-NH2 hydrochloride
  • HY-149574
    Thalidomide-4-O-C12-NH2 hydrochloride
    Thalidomide-4-O-C12-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C12-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-4-O-C12-NH2 hydrochloride
  • HY-149562
    Thalidomide-5-O-C5-NH2 hydrochloride 2761385-94-6
    Thalidomide-5-O-C5-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C5-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C5-NH2 hydrochloride
  • HY-149575
    Thalidomide-4-O-C13-NH2 hydrochloride 99.75%
    Thalidomide-4-O-C13-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C13-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-4-O-C13-NH2 hydrochloride
  • HY-10984R
    Pomalidomide (Standard) 19171-19-8
    Pomalidomide (Standard) is the analytical standard of Pomalidomide. This product is intended for research and analytical applications. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
    Pomalidomide (Standard)
  • HY-155255
    Thalidomide-5-PEG2-NH2 hydrochloride 2761406-70-4
    Thalidomide-5-PEG2-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-PEG2-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-PEG2-NH2 hydrochloride
  • HY-W586822
    N-Methylated pomalidomide 1352827-50-9
    N-methylated pomalidomide (Pomalidomide-methyl), a derivative of Pomalidomide (HY-10984), is a cereblon (CRBN) ligand. N-methylated pomalidomide is unable to recruit CRBN that can be used as a negative control for Pomalidomide. N-methylated pomalidomide can be used to synthesize PROTAC.
    N-Methylated pomalidomide
  • HY-163169
    Phenyl-glutarimide 4'-oxyacetic acid 2782024-58-0
    Phenyl-glutarimide 4 ’-oxyacetic acid is a carboxylic acid-functionalized cerebellar ligand that can be used in the development of PROTAC deactivators. Phenyl-glutarimide 4 ’-oxyacetic acid binds to PROTAC has better hydrolytic stability and efficacy.
    Phenyl-glutarimide 4'-oxyacetic acid
  • HY-W674435
    5-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindole-1,3-dione 2589697-74-3 ≥98.0%
    5-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione is a Thalidomide analogue featuring a hydroxy group, which is a versatile site for further derivitization. Thalidomide is an E3 ligase activator and promotes the ubiquitinylation of a given protein.
    5-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindole-1,3-dione
  • HY-W454678
    5-Bromomethylthalidomide 1312023-72-5
    5-Bromomethylthalidomide is an E3 ligase activator which may be further derivatized by substitution at bromide.
    5-Bromomethylthalidomide
  • HY-10984S4
    Pomalidomide-13C5 1416575-79-5
    Pomalidomide-13C5 (CC-4047-13C5) is 13C labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
    Pomalidomide-<sup>13</sup>C<sub>5</sub>
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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