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-143715
    Cereblon inhibitor 1 2672489-14-2 99.19%
    Cereblon inhibitor 1, an isoindoline derivative, is a cereblon E3 ubiquitin ligase modulating agent. Cereblon inhibitor 1 has the potential for cancer research.
    Cereblon inhibitor 1
  • HY-123324
    Pomalidomide-5-OH 1547162-41-3 99.46%
    Pomalidomide-5-OH (5-hydroxy pomalidomide) is the Pomalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide-5-OH can be connected to the ligand for protein by a linker to form PROTAC.
    Pomalidomide-5-OH
  • HY-10984S1
    Pomalidomide-d3 2093128-28-8 ≥99.0%
    Pomalidomide-d3 is the 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[1][2].
    Pomalidomide-d<sub>3</sub>
  • HY-138040
    CRBN modulator-1 2407829-65-4 98.00%
    CRBN modulator-1, a Thalidomide analog and a CRBN modulator extracted from WO2020006262A1, compound 10, has an IC50 of 3.5 μM and a Ki of 0.98 μM.
    CRBN modulator-1
  • HY-W249500
    2-Methoxyphenyl dihydrouracil 2377643-33-7
    2-Methoxyphenyl dihydrouracil (Compound 13) is a CRBN ligand, and can be used for synthesis of PROTACs.
    2-Methoxyphenyl dihydrouracil
  • HY-46531
    Thalidomide-5-NH2-CH2-COOH 2412056-27-8
    Thalidomide-5-NH2-CH2-COOH (compound 114) is a potent and selective inhibitor of tropomyosin receptor kinase (trk). Thalidomide-5-NH2-CH2-COOH is a ligand of E3 ligase. Thalidomide-5-NH2-CH2-COOH has the potential for researching one or more diseases (extracted from patent WO2021170109A1).
    Thalidomide-5-NH2-CH2-COOH
  • HY-136164
    VH032-OH 2244684-42-0 99.43%
    VH032-OH is the VH032-based VHL ligand. VH032-OH can be connected to the ligand for protein by a linker to form PROTACs.
    VH032-OH
  • HY-129653
    E3 ligase Ligand 18 2241669-88-3 99.22%
    E3 ligase Ligand 18 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 18 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
    E3 ligase Ligand 18
  • HY-W076696
    Lenalidomide-4-OH 1061604-41-8 98.57%
    Lenalidomide-4-OH is the Lenalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Lenalidomide-4-OH can be connected to the ligand for protein by a linker to form PROTAC.
    Lenalidomide-4-OH
  • HY-A0003S
    Lenalidomide-d5 1227162-34-6 99.32%
    Lenalidomide-d5 is deuterium labeled Lenalidomide. Lenalidomide (CC-5013), a derivative of Thalidomide, acts as molecular glue. Lenalidomide is an orally active immunomodulator. Lenalidomide (CC-5013) is a ligand of ubiquitin E3 ligase cereblon (CRBN), and it causes selective ubiquitination and degradation of two lymphoid transcription factors, IKZF1 and IKZF3, by the CRBN-CRL4 ubiquitin ligase. Lenalidomide (CC-5013) specifically inhibits growth of mature B-cell lymphomas, including multiple myeloma, and induces IL-2 release from T cells[1][2].
    Lenalidomide-d<sub>5</sub>
  • HY-43961
    E3 ligase Ligand 8 1225383-33-4 99.32%
    E3 ligase Ligand 8 is a ligand for E3 ubiquitin ligase. E3 ligase Ligand 8 can be connected to the ligand for protein by a linker to form PROTACs. PROTACs are inducers of ubiquitination-mediated degradation of cancer-promoting proteins.
    E3 ligase Ligand 8
  • HY-153661
    Cereblon inhibitor 2 2639380-62-2 98.86%
    Cereblon inhibitor 2 (compound 8) is a Cereblon inhibitor useful in solid tumor research, especially breast cancer.
    Cereblon inhibitor 2
  • HY-139548
    Thalidomide-5-methyl 40313-92-6 99.87%
    Thalidomide-5-methyl is the Thalidomide-based cereblon (CRBN) ligand used in the recruitment of CRBN protein.
    Thalidomide-5-methyl
  • HY-W342590
    CRBN ligand-9 55003-81-1 ≥98.0%
    CRBN ligand-9 (Compound 4d) is a CRBN ligand (Ki: 8.9 μM). CRBN ligand-9 can be used for synthesis of PROTACs.
    CRBN ligand-9
  • HY-132971
    Thalidomide-piperazine hydrochloride 2228029-82-9 98.27%
    Thalidomide-piperazine hydrochloride has the potential for the research of leprosy and multiple myeloma. Thalidomide-piperazine hydrochloride used as a tool in developmental biology leads to important discoveries in the biochemical pathways of limb development.
    Thalidomide-piperazine hydrochloride
  • HY-111823
    VH032 thiol 2098836-54-3
    VH032 thiol (VHL ligand 6) is a VHL ligand, which binds to pan-BET inhibitor JQ1 via a linker to form PROTAC.
    VH032 thiol
  • HY-138678
    (R,S,S)-VH032 2230826-33-0
    (R,S,S)-VH032 is Ligand for E3 Ligase used in the synthesis of PROTACs. VH032 is a VHL ligand and VHL/HIF-1α interaction inhibitor that recruits von Hippel-Lindau (VHL) proteins. (R,S,S)-VH032 synthesizes the tau-targeting small molecule PROTAC C004019 (HY-138669).
    (R,S,S)-VH032
  • HY-144985
    E3 ligase Ligand 23 444287-56-3 99.71%
    E3 ligase Ligand 23 (compound 17-6) is a cereblon binder for the degradation of Ikaros or Aiolos by the ubiquitin proteasome pathway.
    E3 ligase Ligand 23
  • HY-W457950
    Thalidomide-5-propargyl 2226303-74-6
    Thalidomide-5-propargyl is a propargyl-modified Thalidomide (HY-14658), that acts as a Cereblon ligand to recruit CRBN proteins. Thalidomide-5-propargyl use alkynyl group at the end to be directly used in the synthesis of triazoles in the synthesis of PROTAC molecules, and is a key intermediate in the synthesis of PROTAC molecules based on CRBN design.
    Thalidomide-5-propargyl
  • HY-149561
    Thalidomide-5-O-C4-NH2 hydrochloride 2694727-93-8 99.98%
    Thalidomide-5-O-C4-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C4-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C4-NH2 hydrochloride
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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