1. Signaling Pathways
  2. PROTAC
  3. Ligands for E3 Ligase

Ligands for E3 Ligase

E3 ligase-recruiting Moiety

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).

Cat. No. Product Name CAS No. Purity Chemical Structure
  • 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-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-157566
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride 2520105-60-4
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride is a functionalized cerebellar ligand for PROTAC development, combining E3 ligand and terminal piperidine for subsequent chemical reactions. A protein degradant with a rigid connector is generated.
    Lenalidomide 5'-piperazine-4-methylpiperidine hydrochloride
  • 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-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[1][2].
    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[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-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-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-149576
    Thalidomide-4-O-C14-NH2 hydrochloride 99.85%
    Thalidomide-4-O-C14-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C14-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-4-O-C14-NH2 hydrochloride
  • HY-160244
    Pomalidomide 5'-piperazine-4-methylpiperidine dihydrochloride 2758431-93-3 98.08%
    Pomalidomide 5'-piperazine-4-methylpiperidine dihydrochloride is the Pomalidomide (HY-10984)-based cereblon (CRBN) ligand used in the recruitment of CRBN protein. Pomalidomide 5'-piperazine-4-methylpiperidine dihydrochloride can be connected to the ligand for protein by a linker to form PROTAC.
    Pomalidomide 5'-piperazine-4-methylpiperidine dihydrochloride
  • 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
  • HY-W586821
    Thalidomide-1-Me-5-NH2 1468761-60-5 ≥98.0%
    Thalidomide-1-Me-5-NH2 is an aminated Thalidomide analogue. E3 Ligase activators such as this may be used in the design of PROTAC molecules via derivatization at its amine.
    Thalidomide-1-Me-5-NH2
  • HY-W457960
    2-(2,6-Dioxopiperidin-3-yl)-5-ethynylisoindoline-1,3-dione 2154356-63-3
    2-(2,6-Dioxopiperidin-3-yl)-5-ethynylisoindoline-1,3-dione is a Thalidomide analog that can be useful in PROTAC research.
    2-(2,6-Dioxopiperidin-3-yl)-5-ethynylisoindoline-1,3-dione
  • HY-W1004786
    CRBN ligand-13 3050687-70-9
    CRBN ligand-13 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-13
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