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-161191
    Thalidomide-azetidine-piperazine-C2-O-C2-OH
    Thalidomide-azetidine-piperazine-C2-O-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-piperazine-C2-O-C2-OH can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-azetidine-piperazine-C2-O-C2-OH
  • HY-W584534
    VH032-CH2-Boc 2827750-24-1
    VH032-CH2-Boc is a Boc-modified VH032 (HY-120217) that serves as a ligand for VHL and recruits von Hippel-Lindau (VHL) proteins. VH032-CH2-Boc will remove the protecting group under acidic conditions and be directly used in PROTAC molecule synthesis. VH032-CH2-Boc is a key intermediate in the synthesis of PROTAC based on VHL ligand.
    VH032-CH2-Boc
  • HY-P10981
    ErbB2 peptide 325791-52-4
    ErbB2 peptide is a peptide ligand of E3 ubiquitin ligase targeting PI3K for peptide PROTACs.
    ErbB2 peptide
  • HY-168293
    p62-ZZ ligand 1 2409960-13-8
    p62-ZZ ligand 1 (Compound 7) is an p62-ZZ ligand. p62-ZZ ligand 1 can be used for synthesis of VinclozolinM2-2204 (HY-161741).
    p62-ZZ ligand 1
  • HY-168536
    SJ46411 3086104-39-1
    SJ46411 is a potent ligand for KLHDC2, with a Kd of ~260 nM measured by isothermal titration calorimetry (SPR Kd = 0.5 μM, TR-FRET IC50 = 3.9 μM, ΔTm = 6.0 °C).
    SJ46411
  • HY-163229
    (1r,4r)-Thalidomide-piperidine-N(Me)-CH-cyclohexane-NH-Boc
    (1r,4r)-Thalidomide-piperidine-N(Me)-CH-cyclohexane-NH-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1r,4r)-Thalidomide-piperidine-N(Me)-CH-cyclohexane-NH-Boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (1r,4r)-Thalidomide-piperidine-N(Me)-CH-cyclohexane-NH-Boc
  • HY-163221
    (S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-N(Me)-Boc
    (S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-N(Me)-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-N(Me)-Boc 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-(1S,4r)-cyclohexane-N(Me)-Boc
  • HY-168055
    (S)-Deoxy-thalidomide 107657-57-8
    (S)-Deoxy-thalidomide is an E3 ubiquitin ligase ligand. (S)-Deoxy-thalidomide can be linked to the target protein ligand through a linker to form PROTAC K-Ras Degrader-3 (HY-168054). PROTAC K-Ras Degrader-3 can target KRAS mutant proteins for degradation.
    (S)-Deoxy-thalidomide
  • HY-161198
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C-boc
    Thalidomide-azetidine-pyrrolidine-C-piperidine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-pyrrolidine-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-azetidine-pyrrolidine-C-piperidine-C-boc
  • HY-111853
    MV-1-NH-Me 2095244-62-3
    MV-1-NH-Me, the MV-1 based IAP ligand, binds to ABL inhibitor via a linker to form SNIPER.
    MV-1-NH-Me
  • HY-128810
    E3 ligase Ligand 13 2701565-75-3
    E3 ligase Ligand 13 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 13 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 13
  • HY-132944
    (R)-Pomalidomide-pyrrolidine 2418618-52-5
    (R)-Pomalidomide-pyrrolidine, a CRBN ligand, can be connected to the ligand for protein by a linker to form PROTACs.
    (R)-Pomalidomide-pyrrolidine
  • HY-112078A
    (S,R,S,R)-AHPC-Me 2055344-67-5
    (S,R,S,R)-AHPC-Me serves as a VHL ligand that facilitates the recruitment of the VHL protein.
    (S,R,S,R)-AHPC-Me
  • HY-169989
    CRBN ligand-11 2962967-27-5
    CRBN ligand-11 is the E3 ubiquitin ligase ligand for CFT8634 (HY-145925B). CRBN ligand-11 can be used for the synthesis of PROTACs.
    CRBN ligand-11
  • HY-138882A
    Lenalidomide-4-aminomethyl hydrochloride 444289-05-8
    Lenalidomide-4-aminomethyl hydrochloride is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-4-aminomethyl hydrochloride can be connected to the ligand for protein by a linker to form PROTAC
    Lenalidomide-4-aminomethyl hydrochloride
  • HY-161209
    Thalidomide-2,6-diazaspiro[3.4]octane-C-Pip-boc
    Thalidomide-2,6-diazaspiro[3.4]octane-C-Pip-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-Pip-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-Pip-boc
  • HY-172563
    BTR2000
    BTR2000, a specifically KLHL20 ligand, is capable of binding to the KLHL20 Kelch domain with high affinity. BTR2000 can be used as a ligand for E3 ligase for the synthesis of BTR2004 (HY-172562).
    BTR2000
  • HY-163230
    (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc
    (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc can serve as a Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-Boc
  • HY-161183
    (S)-Thalidomide-O-(1S,3r)-C4H4-N(Me)-Pip-C2-O-C-boc
    (S)-Thalidomide-O-(1S,3r)-C4H4-N(Me)-Pip-C2-O-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (S)-Thalidomide-O-(1S,3r)-C4H4-N(Me)-Pip-C2-O-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.
    (S)-Thalidomide-O-(1S,3r)-C4H4-N(Me)-Pip-C2-O-C-boc
  • HY-45808
    Thalidomide-azetidine-CHO 2416132-70-0
    Thalidomide-azetidine-CHO is a synthesized Ligands for E3 Ligase that incorporates the Thalidomide (HY-14658) based cereblon ligand used in PROTAC technology.
    Thalidomide-azetidine-CHO
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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