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-149565
    Thalidomide-5-O-C8-NH2 hydrochloride
    Thalidomide-5-O-C8-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C8-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C8-NH2 hydrochloride
  • HY-149560
    Thalidomide-5-O-C3-NH2 hydrochloride 2694727-94-9 99.08%
    Thalidomide-5-O-C3-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C3-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C3-NH2 hydrochloride
  • HY-163826
    Benzothiazole-CH2(NH-CO-CH2Cl)-CONH-CH2-Ph
    Benzothiazole-CH2(NH-CO-CH2Cl)-CONH-CH2-Ph is a ligand for E3 ubiquitin ligase. Benzothiazole-CH2(NH-CO-CH2Cl)-CONH-CH2-Ph can be connected to the ligand for protein by a linker to form 22-SLF (HY-163807).
    Benzothiazole-CH2(NH-CO-CH2Cl)-CONH-CH2-Ph
  • HY-170108
    CRBN ligand-47 3059455-81-8
    CRBN ligand-47 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-47
  • HY-101291R
    Iberdomide (Standard) 1323403-33-3
    Iberdomide (Standard) is the analytical standard of Iberdomide. This product is intended for research and analytical applications. Iberdomide (CC-220) is an orally active and potent cereblon (CRBN) E3 ligase modulator (CELMoD) with an IC50 of ~150 nM for cereblon-binding affinity. Iberdomide, a derivative of Thalidomide (HY-14658), has antitumor and immunostimulatory activities[1][2].
    Iberdomide (Standard)
  • HY-164043
    (S,R,S)-AHPC(Me)-amido-C2-acid 2365173-01-7
    (S,R,S)-AHPC(Me)-amido-C2-acid is an VHL (E3 ligase) ligand, and can be used for synthesis of PROTACs, such as PROTAC STING Degrader-2 (HY-158036).
    (S,R,S)-AHPC(Me)-amido-C2-acid
  • HY-149572
    Thalidomide-4-O-C9-NH2 hydrochloride
    Thalidomide-4-O-C9-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C9-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-4-O-C9-NH2 hydrochloride
  • HY-W867704
    4-Me-Thalidomide 244057-31-6
    4-Me-Thalidomide is an E3 ligase activator featuring a methyl group. E3 ligase is a protein that marks other proteins for proteolytic destruction by labeling them with ubiquitin.
    4-Me-Thalidomide
  • HY-W898987
    CRBN ligand-83 3036607-28-7
    CRBN ligand-83 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-83
  • HY-156162
    Thalidomide-NH-C14-NH2 hydrochloride
    Thalidomide-NH-C14-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-NH-C14-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).
    Thalidomide-NH-C14-NH2 hydrochloride
  • HY-44249
    Thalidomide-CH2NH2 hydrochloride 444287-40-5
    Thalidomide-CH2NH2 hydrochloride is a Thalidomide analogue featuring a primary amine, which is a versatile group which may participate in many reactions.
    Thalidomide-CH2NH2 hydrochloride
  • HY-172295
    Tetrafluoro-thalidomide 179033-21-7
    Tetrafluoro-thalidomide is a fluorinated Thalidomide analogue. Tetrafluoro-thalidomide is an activator of E3 ligase, which ubiquitinylates proteins for later proteolysis. The structure may be further derivatized via substitution at its fluorines.
    Tetrafluoro-thalidomide
  • HY-173378
    E3 ligase Ligand 59 2913165-27-0
    E3 ligase Ligand 59 (Compound 20e) is the E3 ubiquitin ligase ligand of FDU73 (HY-173125). E3 ligase Ligand 59 can be used to synthesize PROTACs.
    E3 ligase Ligand 59
  • HY-156165
    Thalidomide-5-NH-PEG3-NH2 hydrochloride 2863635-01-0
    Thalidomide-5-NH-PEG3-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-5-NH-PEG3-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).
    Thalidomide-5-NH-PEG3-NH2 hydrochloride
  • HY-42780
    Thalidomide-O-amido-C8-NHBoc 1950635-34-3 98.35%
    Thalidomide-O-amido-C8-NHBoc contains a Thalidomide group, an amide, an alkylC8 chain, and a carbamate protecting group.
    Thalidomide-O-amido-C8-NHBoc
  • HY-W888970
    3-(4-Bromo-2-fluorophenyl)piperidine-2,6-dione 2924092-66-8
    3-(4-Bromo-2-fluorophenyl)piperidine-2,6-dione is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    3-(4-Bromo-2-fluorophenyl)piperidine-2,6-dione
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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