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-162553
    GNE7599 2771069-76-0
    GNE7599 is a high-affinity and orally active von Hippel-Lindau (VHL) ligand with a Kd of 540 pM. GNE7599 can be connected to the ligand for protein by a linker to form PROTACs.
    GNE7599
  • HY-168535
    SJ6145 1010913-79-7
    SJ6145 is a potent ligand for KLHDC2SBD, with the Kd of 16.9 μM in SPR test, IC50 value of 42 μM in inhibiting KLHDC2SBD binding to a di-Gly degron peptide test.
    SJ6145
  • HY-W454906
    tDHU, acid 2377643-37-1
    tDHU, acid is a dihydropyrimidinecereblon ligand that contains an E3 ligase ligand and a benzoic acid linker. tDHU, acid can be used as an E3 ubiquitin ligase ligand-Linker conjugate for the development of PROTACs.
    tDHU, acid
  • HY-161203
    Thalidomide-azetidine-piperazine-C2-O-C-boc
    Thalidomide-azetidine-piperazine-C2-O-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-piperazine-C2-O-C-boc can serve as Cereblon ligand to recruit CRBN protein and serve as a key intermediate for the synthesis of complete PROTAC molecules.
    Thalidomide-azetidine-piperazine-C2-O-C-boc
  • HY-164550
    YF438 2247210-09-7
    YF438 is an HDAC inhibitor with effective anticancer activity both in vitro and in vivo. YF438 inhibits the growth and metastasis of triple-negative breast cancer (TNBC) cells by blocking the interaction between HDAC and MDM2, inducing the dissociation of MDM2-MDMX, and promoting the degradation of MDM2.
    YF438
  • HY-161208
    Deoxy-thalidomide-Pip-C-PIP-boc 2963655-14-1
    Deoxy-thalidomide-Pip-C-PIP-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Deoxy-thalidomide-Pip-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.
    Deoxy-thalidomide-Pip-C-PIP-boc
  • HY-161192
    Thalidomide-O-C4H4-N(Me)-piperidine-C-boc
    Thalidomide-O-C4H4-N(Me)-piperidine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-O-C4H4-N(Me)-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-O-C4H4-N(Me)-piperidine-C-boc
  • HY-169151
    PROTAC BRD4-DCAF1 degrader-1 3036944-87-0
    PROTAC BRD4-DCAF1 degrader-1 (I-907) is a BRD4-DCAF1 PROTAC degrader, DC50 is 10~100 nM. (Pink: BRD4-DCAF1 ligand (HY-169152); Black: linker (HY-126976); Blue: E3 ligase ligand (HY-15846)).
    PROTAC BRD4-DCAF1 degrader-1
  • HY-163225
    (S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-NH-Boc
    (S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-NH-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-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.
    (S)-Thalidomide-piperazine-(1S,4r)-cyclohexane-NH-Boc
  • HY-161205
    Thalidomide-PIP-(R)C-pyrrolidine-boc 2839668-87-8
    Thalidomide-PIP-(R)C-pyrrolidine-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-PIP-(R)C-pyrrolidine-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-PIP-(R)C-pyrrolidine-boc
  • HY-161184
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Deoxy-thalidomide-piperidine-C-piperazine-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.
    Deoxy-thalidomide-piperidine-C-piperazine-C2-OH
  • HY-131189
    N-Boc-SBP-0636457-OH 2450350-79-3
    N-Boc-SBP-0636457-OH, a ligand for E3 ubiquitin ligase, is used in the recruitment of IAP E3 ligases. N-Boc-SBP-0636457-OH can be connected to the ligand for Bcl-xL by a linker to form PROTAC Bcl-xL degrader-1 (HY-131188).
    N-Boc-SBP-0636457-OH
  • HY-W595340
    E3 ubiquitin ligase binder-1 2446913-99-9
    E3 ubiquitin ligase binder-1 (compound 11) is a potent E3 ubiquitin ligase binder. E3 ubiquitin ligase binder-1 is a ligand for E3 Ligase.
    E3 ubiquitin ligase binder-1
  • HY-159597
    Thalidomide-methylpyrrolidine 2616540-84-0
    Thalidomide-methylpyrrolidine is a ligand for E3 ubiquitinase. Thalidomide-methylpyrrolidine can be used to synthesize CW-3308 (HY-159579).
    Thalidomide-methylpyrrolidine
  • HY-161202
    Thalidomide-piperidine-O-piperidine-C2-OH
    Thalidomide-piperidine-O-piperidine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperidine-O-piperidine-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-piperidine-O-piperidine-C2-OH
  • 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-W584516
    Thalidomide-5-NH-CH2-COO(t-Bu) 2412056-28-9
    Thalidomide-5-NH-CH2-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-5-NH-CH2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-5-NH-CH2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
    Thalidomide-5-NH-CH2-COO(t-Bu)
  • HY-400254
    cis VH032 amine dihydrochloride 2376990-32-6
    cis VH032 amine dihydrochloride is a VHL ligand with a Ki of 5.7 μM. cis VH032 amine dihydrochloride can be used to regulate hypoxia signaling pathways and to study chronic anemia or ischemia.
    cis VH032 amine dihydrochloride
  • HY-161206
    Thalidomide-Pip-C-Pip-O-C-boc
    Thalidomide-Pip-C-Pip-O-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-Pip-C-Pip-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.
    Thalidomide-Pip-C-Pip-O-C-boc
  • HY-163951
    (S,R,S)-AHPC-Ac 2361116-63-2
    (S,R,S)-AHPC-Ac is a ligand for E3 ubiquitinase. (S,R,S)-AHPC-Ac can be used to synthesize PROTAC SMARCA2/4-degrader-22 (HY-163875).
    (S,R,S)-AHPC-Ac
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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