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-W460141
    Thalidomide 4-chloro 244057-36-1 99.74%
    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-W1130394
    Thalidomide-O-amido-PEG2-Mal
    Thalidomide-O-amido-PEG2-Mal is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. Thalidomide-O-amido-PEG2-Mal can be linked to a target protein ligand via a linker to form a PROTAC.
    Thalidomide-O-amido-PEG2-Mal
  • HY-W763812
    (S)-Thalidomide 4-fluoride 911109-85-8
    (S)-Thalidomide 4-fluoride is a CRBN E3 ligase ligand that can be used for synthesis of DeDPP4 (HY-182336).
    (S)-Thalidomide 4-fluoride
  • HY-W441376
    Thalidomide-1-Me,4-OH 2244568-06-5 ≥98.0%
    Thalidomide-1-Me,4-OH is a Thalidomide (HY-14658) analogue. Thalidomide-1-Me,4-OH contains an extra methyl group on the glutarimide moiety of thalidomide, which is known to abrogate its ability to bind the E3 ligase CRBN. Thalidomide is a ligand for E3 ligase, which ubiquitinylates proteins, thus committing their fate to proteolytic destruction.
    Thalidomide-1-Me,4-OH
  • HY-170108
    CRBN ligand-47 3059455-81-8 99.93%
    CRBN ligand-47 is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    CRBN ligand-47
  • HY-44249
    Thalidomide-CH2NH2 hydrochloride 444287-40-5 98.06%
    Thalidomide-CH2NH2 hydrochloride is a Thalidomide analogue featuring a primary amine, which is a versatile group which may participate in many reactions.
    Thalidomide-CH2NH2 hydrochloride
  • HY-W248665
    Thalidomide-pyrrolidine 2616540-83-9
    Thalidomide-pyrrolidine is an E3 ligase ligand. Thalidomide-pyrrolidine can be used for synthesis of PROTAC ARD-1676 (HY-156111).
    Thalidomide-pyrrolidine
  • HY-W575237
    Desamino lenalidomide-NO2 1198787-23-3 99.76%
    Desamino lenalidomide-NO2 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. Desamino lenalidomide-NO2 can be linked to a target protein ligand via a linker to form a PROTAC.
    Desamino lenalidomide-NO2
  • HY-W888970
    3-(4-Bromo-2-fluorophenyl)piperidine-2,6-dione 2924092-66-8 98.55%
    3-(4-Bromo-2-fluorophenyl)piperidine-2,6-dione is a CRBN-type E3 ubiquitin ligase ligand that can be used to prepare PROTAC.
    3-(4-Bromo-2-fluorophenyl)piperidine-2,6-dione
  • HY-W867177
    CRBN ligand-617 2713620-89-2
    CRBN ligand-617 is an E3 ubiquitin ligase cereblon (CRBN) ligand used to recruit the cereblon protein. CRBN ligand-617 can be linked to a target protein ligand via a linker to form a PROTAC.
    CRBN ligand-617
  • HY-10984S2
    Pomalidomide-d4 1416575-78-4
    Pomalidomide-d4 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>4</sub>
  • HY-172563A
    BTR2000 TFA 98.95%
    BTR2000 TFA, a specifically KLHL20 ligand, is capable of binding to the KLHL20 Kelch domain with high affinity. BTR2000 TFA can be used as a ligand for E3 ligase for the synthesis of BTR2004 (HY-172562).
    BTR2000 TFA
  • 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-W584986
    Thalidomide-(2)piperidine 2616553-33-2 99.42%
    Thalidomide-(2)piperidine (compound 9) is a potent E3 ligase ligand. Thalidomide-(2)piperidine can be used for synthesis of PROTACs.
    Thalidomide-(2)piperidine
  • HY-W248665A
    Thalidomide-pyrrolidine hydrochloride 2616553-35-4 98.0%
    Thalidomide-pyrrolidine hydrochloride (Compound 18) is an E3 ligase ligand. Thalidomide-pyrrolidine serves as a building block for the synthesis of PROTAC ARD-1676 (HY-156111).
    Thalidomide-pyrrolidine hydrochloride
  • HY-150825
    CST530 847137-53-5
    CST530 is an inhibitor of apoptosis protein (IAP) antagonist. CST530 is an IAP-type Ligands for E3 Ligase. CST530 binds to the BIR3 domain of IAP and interferes with its function, thereby promoting the ubiquitination and degradation of cIAP1. CST530 can be used to prepare PROTACs.
    CST530
  • 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 98.71%
    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
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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