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-W244282
    Thalidomide-pinacolborane 2229725-98-6
    Thalidomide-pinacolborane is a Thalidomide analogue featuring a boronic pinacol ester, otherwise known as a Bpin group, and they are most frequently used in Suzuki reactions. This molecule is an activator for E3 ligase, which ubiquitinylates proteins, thus committing their fate to proteolytic destruction.
    Thalidomide-pinacolborane
  • HY-A0003BR
    Lenalidomide hemihydrate (Standard) 847871-99-2
    Lenalidomide (hemihydrate) (Standard) is the analytical standard of Lenalidomide (hemihydrate). This product is intended for research and analytical applications. Lenalidomide hemihydrate (CC-5013 hemihydrate), a derivative of Thalidomide, acts as molecular glue. Lenalidomide hemihydrate is an orally active immunomodulator. Lenalidomide hemihydrate (CC-5013 hemihydrate) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide hemihydrate (CC-5013 hemihydrate) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells.
    Lenalidomide hemihydrate (Standard)
  • HY-163826
    Benzothiazole-CH2(NH-CO-CH2Cl)-CONH-CH2-Ph 3079209-79-0
    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.
    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-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-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-176045
    LC3B ligand 2
    LC3B ligand 2 is a ligand for E3 ubiquitin ligase. LC3B ligand 2 can be connected to the ligand for protein by a linker to form PROTAC PCSK9 autophagic degrader 2 (HY-176043). PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
    LC3B ligand 2
  • 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-172955
    E3 ligase Ligand 65 2417258-70-7
    E3 ligase Ligand 65 is a ligand for E3 ligase, used for the synthesis of AZ'3137 (HY-162702) .
    E3 ligase Ligand 65
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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