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-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-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
  • HY-161195
    Deoxy-thalidomide-piperidine-C-piperazine-C-boc
    Deoxy-thalidomide-piperidine-C-piperazine-C-boc is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Deoxy-thalidomide-piperidine-C-piperazine-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.
    Deoxy-thalidomide-piperidine-C-piperazine-C-boc
  • HY-W584517
    Thalidomide-5-O-CH2-COO(t-Bu) 2682112-10-1
    Thalidomide-5-O-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-O-CH2-COO(t-Bu) can be removed under acidic conditions to participate in the synthesis of PROTAC molecules. Thalidomide-5-O-CH2-COO(t-Bu) is a key intermediate in the synthesis of CRBN-based PROTAC molecules.
    Thalidomide-5-O-CH2-COO(t-Bu)
  • HY-161367
    VHL-SF2 3050690-24-6
    VHL-SF2 is a VHL ligand, and can be used for synthesis of PROTACs
    VHL-SF2
  • HY-149935
    OICR-8268 3000549-26-5
    OICR-8268 is a reversible DCAF1 ligand that binds to the DCAF1 WDR domain with a Kd of 38 nM. OICR-8268 can enable the development of DCAF1-based PROTACs.
    OICR-8268
  • HY-128809
    cIAP1 ligand 2 2357114-70-4
    cIAP1 ligand 2 is the LCL161 derivative based IAP ligand. cIAP1 ligand 2 can be connected to the ABL ligand for protein by a linker to form SNIPER.
    cIAP1 ligand 2
  • HY-150799
    CRBN ligand-1 3032314-67-0
    CRBN ligand-1 is a ligand for E3 ligase.
    CRBN ligand-1
  • HY-139547
    Thalidomide-5,6-Cl 2648939-40-4
    Thalidomide-5,6-Cl is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-5,6-Cl can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5,6-Cl
  • HY-10984S3
    Pomalidomide-15N,13C5
    Pomalidomide-15N,13C5 is 15N and 13C labeled Pomalidomide (HY-10984). 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-<sup>15</sup>N,<sup>13</sup>C<sub>5</sub>
  • HY-139540
    Pomalidomide-6-OH 1547162-44-6 98.09%
    Pomalidomide-6-OH is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-6-OH can be connected to the ligand for protein by a linker to form PROTAC.
    Pomalidomide-6-OH
  • HY-139656
    cIAP1 ligand 4 2891589-73-2
    cIAP1 ligand 4 is a ligand for E3 ligase that can be used in the synthesis of PROTACs.
    cIAP1 ligand 4
  • HY-139542
    Pomalidomide-6-O-CH3 1547163-08-5
    Pomalidomide-6-O-CH3 is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-6-O-CH3 can be connected to the ligand for protein by a linker to form PROTAC.
    Pomalidomide-6-O-CH3
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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