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-163169
    Phenyl-glutarimide 4'-oxyacetic acid 2782024-58-0
    Phenyl-glutarimide 4 ’-oxyacetic acid is a carboxylic acid-functionalized cerebellar ligand that can be used in the development of PROTAC deactivators. Phenyl-glutarimide 4 ’-oxyacetic acid binds to PROTAC has better hydrolytic stability and efficacy.
    Phenyl-glutarimide 4'-oxyacetic acid
  • HY-W674435
    5-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindole-1,3-dione 2589697-74-3 ≥98.0%
    5-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione is a Thalidomide analogue featuring a hydroxy group, which is a versatile site for further derivitization. Thalidomide is an E3 ligase activator and promotes the ubiquitinylation of a given protein.
    5-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindole-1,3-dione
  • HY-W454678
    5-Bromomethylthalidomide 1312023-72-5
    5-Bromomethylthalidomide is an E3 ligase activator which may be further derivatized by substitution at bromide.
    5-Bromomethylthalidomide
  • HY-10984S4
    Pomalidomide-13C5 1416575-79-5
    Pomalidomide-13C5 (CC-4047-13C5) is 13C 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-<sup>13</sup>C<sub>5</sub>
  • HY-156163
    Thalidomide-5-NH-PEG1-NH2 hydrochloride 2863634-98-2
    Thalidomide-5-NH-PEG1-NH2 hydrochloride is a Thalidomide (HY-14658)-based cereblon ligand that recruits CRBN proteins. Thalidomide-5-NH-PEG1-NH2 hydrochloride can be connected to the target protein ligand through a linker to form a PROTAC molecule. For example, THAL-SNS-032 (HY-123937).
    Thalidomide-5-NH-PEG1-NH2 hydrochloride
  • HY-W458018
    Thalidomide-4-Br,7-F 2740657-30-9
    Thalidomide-4-Br,7-F is an E3 ligase activator featuring a bromine and a fluorine. E3 ligase is a protein that marks other proteins for proteolytic destruction by labeling them with ubiquitin. Both halogens may be substituted for further derivitization.
    Thalidomide-4-Br,7-F
  • HY-A0003S3
    Lenalidomide-d4 1130061-52-7
    Lenalidomide-d4 (CC-5013-d4) 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>4</sub>
  • HY-171224
    CRBN ligand-45 3065496-78-5
    CRBN ligand-45 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-45
  • HY-168535
    SJ6145 1010913-79-7
    SJ6145 is a potent ligand for KLHDC2SBD, with the Kd of 16.9 μM in SPR test, IC50 value of 42 μM in inhibiting KLHDC2SBD binding to a di-Gly degron peptide test.
    SJ6145
  • HY-W898991
    CRBN ligand-112 3036607-49-2
    CRBN ligand-112 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-112
  • HY-170126
    CRBN ligand-74 3065251-87-5
    CRBN ligand-74 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-74
  • HY-170075
    CRBN ligand-16 3050687-81-2
    CRBN ligand-16 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-16
  • HY-170131
    CRBN ligand-84 3065251-76-2
    CRBN ligand-84 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-84
  • HY-155257
    Thalidomide-5-PEG7-NH2 hydrochloride
    Thalidomide-5-PEG7-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-PEG7-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-PEG7-NH2 hydrochloride
  • HY-149571
    Thalidomide-5-O-C14-NH2 hydrochloride
    Thalidomide-5-O-C14-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C14-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C14-NH2 hydrochloride
  • HY-149573
    Thalidomide-4-O-C11-NH2 hydrochloride 99.94%
    Thalidomide-4-O-C11-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C11-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-4-O-C11-NH2 hydrochloride
  • HY-149559
    Thalidomide-5-O-C2-NH2 hydrochloride 2694727-89-2 98.01%
    Thalidomide-5-O-C2-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C2-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C2-NH2 hydrochloride
  • HY-156160
    Thalidomide-NH-C10-NH2 hydrochloride 2460022-53-9
    Thalidomide-NH-C10-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-NH-C10-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-NH-C10-NH2 hydrochloride
  • HY-159465
    E3 ligase Ligand 30 2725913-42-6
    E3 ligase Ligand 30 is a ligand for E3 ligase.
    E3 ligase Ligand 30
  • HY-W244282
    Thalidomide-pinacolborane 2229725-98-6
    Thalidomide-pinacolborane is a Thalidomide analogue featuring a boronic pinacol ester, otherwise known as a Bpin group, and they are most frequently used in Suzuki reactions. This molecule is an activator for E3 ligase, which ubiquitinylates proteins, thus committing their fate to proteolytic destruction.
    Thalidomide-pinacolborane
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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