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-168699
    E3 ligase Ligand 45
    E3 ligase Ligand 45 is an E3 ligase ligand that can be used to synthesize the PROTAC degrader Setidegrasib (HY-148273) for Ras.
    E3 ligase Ligand 45
  • HY-163238
    Thalidomide-azetidine-CH-piperazineethanol
    Thalidomide-azetidine-CH-piperazineethanol is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-azetidine-CH-piperazineethanol 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-CH-piperazineethanol
  • HY-W584527
    VH032 analogue-1 2111829-84-4
    VH032 analogue-1 is a VH032 (HY-120217) analog that acts as a ligand for VHL, recruiting von Hippel-Lindau (VHL) protein. VH032 analogue-1 will remove the protective group under acidic conditions and be directly used for PROTAC molecular synthesis. VH032 analogue-1 is a key intermediate in the synthesis of PROTACs based on VHL ligands.
    VH032 analogue-1
  • HY-161415
    BCL-xL/BCL-2 ligand 1 2941091-91-2
    BCL-xL/BCL-2 ligand 1 (compound 72-1) is a BCL-xL and BCL-2 protein ligand. BCL-xL/BCL-2 ligand 1 can be connected to the E3 ligase by a linker to form PROTACs (HY-161410).
    BCL-xL/BCL-2 ligand 1
  • HY-161770
    HL389
    HL389 inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389 can be utilized as the ligand for E3 ligase for the synthesis of PROTAC degrader HL435 (HY-161769).
    HL389
  • HY-161190
    Thalidomide-piperidine-C-2,6-diazaspiro[3.3]heptane-C2-OH
    Thalidomide-piperidine-C-2,6-diazaspiro[3.3]heptane-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperidine-C-2,6-diazaspiro[3.3]heptane-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-C-2,6-diazaspiro[3.3]heptane-C2-OH
  • HY-139549
    Thalidomide-benzo 458151-34-3
    Thalidomide-benzo hydrochloride is the Thalidomide-based cereblon ligand used in the recruitment of CRBN protein. Thalidomide-benzo can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-benzo
  • HY-W797329
    (3S)Lenalidomide-5-Br 2829898-76-0
    (3S)Lenalidomide-5-Br is a ligand for E3 ubiquitinase. (3S)Lenalidomide-5-Br can be used to synthesize PROTAC Cbl-b-IN-1 (HY-159608).
    (3S)Lenalidomide-5-Br
  • HY-161197
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH
    Thalidomide-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH 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-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-2,6-diazaspiro[3.4]octane-C-piperidine-C2-O-C2-OH
  • HY-W584525
    VH032-NH-CO-CH2-NHBoc 2010986-19-1
    VH032-NH-CO-CH2-NHBoc is a Boc-modified VH032 (HY-120217) that acts as a ligand for VHL to recruit von Hippel-Lindau (VHL) proteins. VH032-NH-CO-CH2-NHBoc will remove the Boc protection under acidic conditions, and connect with the target protein ligand through a linker to form a PROTAC molecule, which is a key intermediate for the synthesis of PROTAC based on VHL ligand.
    VH032-NH-CO-CH2-NHBoc
  • HY-172948
    VHL Ligand 36 2250056-48-3
    VHL Ligand 36 is a von Hippel-Lindau (VHL) ligand. VHL Ligand 36 can be used to synthesize SD-2301 (HY-172946).
    VHL Ligand 36
  • HY-161188
    Thalidomide-O-C4H4-N(Me)-piperidine-C2-OH
    Thalidomide-O-C4H4-N(Me)-piperidine-C2-OH is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-O-C4H4-N(Me)-piperidine-C2-OH can serve as 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-C2-OH
  • HY-163237
    Thalidomide-piperidine-O-azetidineethanol
    Thalidomide-piperidine-O-azetidineethanol is a conjugate of E3 ligase ligand and linker, consisting of Thalidomide (HY-14658) and the corresponding Linker. Thalidomide-piperidine-O-azetidineethanol 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-azetidineethanol
  • HY-170126S
    9-Amino-1,2,3,4-tetrahydroacridin-1-ol-d3 Maleate 1219806-48-0
    9-Amino-1,2,3,4-tetrahydroacridin-1-ol-d3 Maleate is the deuterium labeled CRBN ligand-74 (HY-170126). CRBN ligand-74 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    9-Amino-1,2,3,4-tetrahydroacridin-1-ol-d<sub>3</sub> Maleate
  • 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-W454906
    tDHU, acid 2377643-37-1 98.83%
    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-W890189
    E3 ligase Ligand 54 2413038-90-9
    E3 ligase Ligand 54 is the ligand for E3 ligase Cereblon and can be used for synthesis of PROTAC Degrader SJ44236 (HY-170900).
    E3 ligase Ligand 54
  • HY-157558
    KDRLKZ-1
    KDRLKZ-1 is a KLHDC2 ligand (Kd = 0.36 μM), with IC50s of 0.21 μM and 0.31 μM in alphaLISA and time-resolved fluorescence resonance energy transfer (TR-FRET) displacement assays.
    KDRLKZ-1
  • 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-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
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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