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-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-W733176
    E3 ligase Ligand 50 2758531-98-3
    E3 ligase Ligand 50 is the ligand for E3 ligase Cereblon. E3 ligase Ligand 50 can be used for synthesis of PROTAC BTK Degrader-10 (HY-160966).
    E3 ligase Ligand 50
  • HY-W957284
    DCAF11 ligand 1 2940939-13-7
    DCAF11 ligand 1 is the ligand for E3 ligase DCAF11 and can be used for PROTAC synthesis of FF2039 (HY-172159).
    DCAF11 ligand 1
  • HY-157512
    SJF-0661 2413035-43-3
    SJF-0661 is a variant of the von Hippel-Lindau (VHL) protein ligand with no targeted degradation ability and can be used as a control reagent for the VHL ubiquitin ligase ligand. SJF-0661 is a variant obtained by inverting the stereocenter of the key hydroxyproline group in the VHL ligand.
    SJF-0661
  • 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
  • HY-161186
    Thalidomide-piperidine-C-azetidine-C2-O-C-boc
    Thalidomide-piperidine-C-azetidine-C2-O-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperidine-C-azetidine-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.
    Thalidomide-piperidine-C-azetidine-C2-O-C-boc
  • HY-163227
    (1R,4R)-Thalidomide-2,5-diazabicyclo[2.2.1]heptane-(1R,4r)-cyclohexane-NH-Boc
    (1R,4R)-Thalidomide-2,5-diazabicyclo[2.2.1]heptane-(1R,4r)-cyclohexane-NH-Boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. (1R,4R)-Thalidomide-2,5-diazabicyclo[2.2.1]heptane-(1R,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.
    (1R,4R)-Thalidomide-2,5-diazabicyclo[2.2.1]heptane-(1R,4r)-cyclohexane-NH-Boc
  • HY-10984S
    Pomalidomide-d5 1377838-49-7
    Pomalidomide-d5 is deuterium labeled Pomalidomide. Pomalidomide, the third-generation immunomodulatory agent, acts as molecular glue. Pomalidomide interacts with the E3 ligase cereblon and induces degradation of essential Ikaros transcription factors.
    Pomalidomide-d<sub>5</sub>
  • HY-161187
    Thalidomide-piperidine-1,6-diazaspiro[3.3]heptane-boc
    Thalidomide-piperidine-1,6-diazaspiro[3.3]heptane-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperidine-1,6-diazaspiro[3.3]heptane-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-piperidine-1,6-diazaspiro[3.3]heptane-boc
  • HY-161189
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C-boc
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C-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-piperidine-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-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C-boc
  • HY-162855
    E3 ligase Ligand 33 3023410-43-4
    E3 ligase Ligand 33 (56-9B) is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 33 can be used in anti-cancer research.
    E3 ligase Ligand 33
  • HY-163932
    (S,R,S)-AHPC-O-CF3 2641373-92-2
    (S,R,S)-AHPC-O-CF3 is a ligand for E3 ubiquitinase. (S,R,S)-AHPC-O-CF3 can be used to synthesize PROTAC SMARCA2/4-degrader-20 (HY-163873).
    (S,R,S)-AHPC-O-CF3
  • HY-101763B
    (S,R,S)-AHPC dihydrochloride 2137142-47-1
    (S,R,S)-AHPC (VH032-NH2) dihydrochloride is the VH032-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein. (S,R,S)-AHPC dihydrochloride can be connected to the ligand for protein (e.g., BCR-ABL1) by a linker to form PROTACs (e.g., GMB-475). GMB-475 induces the degradation of BCR-ABL1 with an IC50 of 1.11 μM in Ba/F3 cells.
    (S,R,S)-AHPC dihydrochloride
  • HY-168232
    E3 ligase Ligand 35
    E3 ligase Ligand 35 serves as the E3 ligase ligand for PROTAC SMARCA2 degrader-27 (HY-168229).
    E3 ligase Ligand 35
  • HY-168646
    SJ46411-Br
    SJ46411-Br is one of CRL2KLHDC2 targeting Ligands for E3 Ligase. SJ46411-Br can bind to KLHDC2 to form a complex to promote cooperative homologous selective ternary complex formation. SJ46411-Br can be coupled to BET ligand JQ1 (HY-13030) through PROTAC linker to synthesize corresponding PROTACs.
    SJ46411-Br
  • HY-401613
    E3 ligase Ligand 43 2821795-71-3
    E3 ligase Ligand 43 serves as the E3 ubiquitin ligase ligand for ACBI3 (HY-157228). E3 ligase Ligand 43 can be utilized for the synthesis of PROTACs.
    E3 ligase Ligand 43
  • HY-159076
    E3 ligase Ligand 7 37630-54-9
    E3 ligase Ligand 7 (Compound 6) is a ligand for E3 ligase. E3 ligase Ligand 7 can be utilized for the synthesis of PROTAC BET Degrader-12 (HY-158764).
    E3 ligase Ligand 7
  • HY-157749
    Thalidomide-piperazine-(S)-CH2-pyrrolidine-C2-O-CH2-COO-C(CH3)3
    Thalidomide-piperazine-(S)-CH2-Pyrrolidine-C2-O-CH2-COO-C (CH3)3 is a synthetic E3 ligase ligand-Linker conjugate. Thalidomide-piperazine-(S)-Ch2-Pyrrolidine-C2-O-CH2-COO-C(CH3)3 includes Thalidomide-based cereblon ligands and linkers. Thalidomide-piperazine-(S)-CH2-Pyrrolidine-C2-O-CH2-COO-C(CH3)3 can be used to synthesize PROTAC BET.
    Thalidomide-piperazine-(S)-CH2-pyrrolidine-C2-O-CH2-COO-C(CH3)3
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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