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-153215
    MEL24 642072-48-8 ≥98.0%
    MEL24 is an Mdm2 E3 ligase inhibitor that reduces cell survival and increases sensitivity to DNA damaging agents in a p53-dependent manner for in vitro antitumor studies.
    MEL24
  • 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-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-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.
    Pomalidomide-d<sub>3</sub>
  • 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-W039233
    Lenalidomide-F 2359705-88-5 99.89%
    Lenalidomide-F is a E3 ligase ligand for LWY713. LWY713 is a PROTAC-class FLT3 degrader (DC50 = 0.64 nM), which selectively induces FLT3 degradation via cereblon and proteasome-dependent pathways.
    Lenalidomide-F
  • HY-W460141
    Thalidomide 4-chloro 244057-36-1
    Thalidomide 4-chloro is a chlorinated E3 ligase activator. Thalidomide 4-chloro may be used for further derivitization by substitution of chlorine.
    Thalidomide 4-chloro
  • 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-W248665A
    Thalidomide-pyrrolidine hydrochloride 2616553-35-4 ≥98.0%
    Thalidomide-pyrrolidine hydrochloride (compound 18) is an E3 ligase ligand, and can be used for synthesis of PROTACs.
    Thalidomide-pyrrolidine hydrochloride
  • HY-150839
    E3 ligase Ligand PG 14149-34-9 99.94%
    E3 ligase Ligand PG is a E3 ligase ligand that can be used in the recruitment of CRBN protein. E3 ligase Ligand PG exhibits potent binding activity with CRBN (IC50 of 2.191 μM). E3 ligase Ligand PG can be connected to the BMS-202 (HY-19745) by a linker to form PROTAC, PROTAC PD-L1 degrader-1 (HY-163757).
    E3 ligase Ligand PG
  • 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-14658S
    Thalidomide-d4 1219177-18-0 98.00%
    Thalidomide-d4 is a deuterium labeled Thalidomide. Thalidomide inhibits cereblon (CRBN), a part of the cullin-4 E3 ubiquitin ligase complex CUL4-RBX1-DDB1, with a Kd of ~250 nM, and has immunomodulatory, anti-inflammatory and anti-angiogenic cancer properties.
    Thalidomide-d<sub>4</sub>
  • 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.
    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 (HY-14658)-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Thalidomide-5-methyl can be used to synthesize PROTAC.
    Thalidomide-5-methyl
  • 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
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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