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-138882
    Lenalidomide-4-aminomethyl 790652-68-5
    Lenalidomide-4-aminomethyl is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-4-aminomethyl can be connected to the ligand for protein by a linker to form PROTAC.
    Lenalidomide-4-aminomethyl
  • HY-148834
    Pomalidomide-piperazine 2154342-57-9
    Pomalidomide-piperazine is an active compound that can be used to synthesis the E3 ligand for PROTAC.
    Pomalidomide-piperazine
  • HY-111850
    Bestatin-amido-Me 339186-54-8
    Bestatin-amido-Me, the Bestatin-based IAP ligand, binds to ABL inhibitor via a linker to form SNIPER.
    Bestatin-amido-Me
  • HY-159660
    E3 ligase Ligand 31 2357114-13-5
    E3 ligase Ligand 31 is a ligand for E3 ubiquitinase. E3 ligase Ligand 31 can be used to synthesize PTOTAC HSD17B13 degrader 1 (HY-159651).
    E3 ligase Ligand 31
  • HY-159547
    Cyclopropane-(S,R,S)-AHPC 2502205-74-3
    E3 ligase Ligand 30 is a ligand for E3 ligase.
    Cyclopropane-(S,R,S)-AHPC
  • HY-100947A
    cis VH-298 2097381-86-5
    cis VH-298 is a cis-form of VH-298 (HY-100947). VH-298 is a highly potent inhibitor of the VHL:HIF-α interaction with a Kd value of 80 to 90 nM, used in PROTAC technology.
    cis VH-298
  • HY-158678
    E3 ligase Ligand 27 3034204-25-3
    E3 ligase Ligand 27 (part of 15) is a ligand for E3 ligase, used for the synthesis of PROTAC BcI-2/BcI-xI Degrader-1 (HY-158551)
    E3 ligase Ligand 27
  • HY-W584528
    VH032 analogue-2 1448189-66-9
    VH032 analogue-2 is a VH032 (HY-120217) analog that acts as a ligand for VHL, recruiting von Hippel-Lindau (VHL) protein. VH032 analogue-2 will remove the protective group under acidic conditions, and can be directly used for the synthesis of PROTAC molecules. VH032 analogue-2 is a key intermediate for the synthesis of PROTACs based on VHL ligands.
    VH032 analogue-2
  • HY-W584513
    Thalidomide-NH-(CH2)2-NH-Boc 1957235-57-2
    Thalidomide-NH-(CH2)2-NH-Boc is a Boc-modified Thalidomide (HY-14658) that acts as a Cereblon ligand to recruit CRBN protein. The Boc protecting group at the end of Thalidomide-NH-(CH2)2-NH-Boc can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-NH-(CH2)2-NH-Boc is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
    Thalidomide-NH-(CH2)2-NH-Boc
  • HY-161637
    E3 ligase Ligand 25 2633633-39-1
    E3 ligase Ligand 25 (part of Compd 1) is a ligand for E3 ligase, used for the synthesis of PROTAC SOS1 degrader (HY-161634).
    E3 ligase Ligand 25
  • HY-163226
    (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-(1R,4r)-cyclohexane-NH-Boc
    (1R,5S)-Thalidomide-3,8-diazabicyclo[3.2.1]octane-(1R,4r)-cyclohexane-NH-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-(1R,4r)-cyclohexane-NH-Boc can serve as 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-(1R,4r)-cyclohexane-NH-Boc
  • HY-157760
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-OH
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-OH can serve as a Cereblon ligand to recruit CRBN proteins and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    (S)-Thalidomide-piperazine-pyrimidine-piperazine-C2-OH
  • HY-144980
    E3 ligase Ligand 21 2504233-73-0
    E3 ligase Ligand 21 (compound 2) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway.
    E3 ligase Ligand 21
  • 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-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-W584524
    Thalidomide-4-NH-PEG2-COO(t-Bu) 2140807-16-3
    Thalidomide-4-NH-PEG2-COO(t-Bu) is a t-Bu modified Thalidomide (HY-14658), which acts as a Cereblon ligand to recruit CRBN protein. The t-Bu protecting group at the end of Thalidomide-4-NH-PEG2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-4-NH-PEG2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
    Thalidomide-4-NH-PEG2-COO(t-Bu)
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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