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-W877989
    BWA-522 intermediate-1 2241315-66-0 99.27%
    BWA-522 intermediate-1 is an intermediate in the synthesis of PROTAC BWA-522 (HY-149433) and serves as a ligand molecule for cereblon E3 ubiquitin ligase. BWA-522 is an orally active small molecule protein-targeting chimera (PROTAC) that has significant degradation effects on AR-FL and AR-V7.
    BWA-522 intermediate-1
  • HY-149564
    Thalidomide-5-O-C7-NH2 hydrochloride 98.13%
    Thalidomide-5-O-C7-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C7-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C7-NH2 hydrochloride
  • HY-149574
    Thalidomide-4-O-C12-NH2 hydrochloride
    Thalidomide-4-O-C12-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C12-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-4-O-C12-NH2 hydrochloride
  • HY-149562
    Thalidomide-5-O-C5-NH2 hydrochloride 2761385-94-6
    Thalidomide-5-O-C5-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-O-C5-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-O-C5-NH2 hydrochloride
  • HY-149575
    Thalidomide-4-O-C13-NH2 hydrochloride 99.75%
    Thalidomide-4-O-C13-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-4-O-C13-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-4-O-C13-NH2 hydrochloride
  • HY-10984R
    Pomalidomide (Standard) 19171-19-8
    Pomalidomide (Standard) is the analytical standard of Pomalidomide. This product is intended for research and analytical applications. 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 (Standard)
  • HY-155255
    Thalidomide-5-PEG2-NH2 hydrochloride 2761406-70-4
    Thalidomide-5-PEG2-NH2 hydrochloride is the Thalidomide (HY-10984)-based cereblon ligand used in the recruitment of CRBN protein.Thalidomide-5-PEG2-NH2 hydrochloride can be connected to the ligand for protein by a linker to form PROTACs.
    Thalidomide-5-PEG2-NH2 hydrochloride
  • HY-161770
    HL389
    HL389 inhibits proliferation of cancer cells MDA-MB-231 and MCF-7, with IC50 of 11.39 μM and 9.66 μM. HL389 can be utilized as the ligand for E3 ligase for the synthesis of PROTAC degrader HL435 (HY-161769).
    HL389
  • 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-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-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-163210
    Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride 2758431-94-4
    Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride (ZJT1) is an E3 ubiquitin ligase cereblon based on Pomalidomide (HY-10984) (CRBN) ligand for recruitment of cereblon protein. Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride can be linked to protein ligand by linker to form PROTAC.
    Pomalidomide 5'-fluoro-6'-piperazine-4-methylpiperidine hydrochloride
  • HY-120520
    Caylin-1 1207480-88-3
    Caylin-1 is an inhibitor of MDM2 and an analog of Nutlin-3. Caylin-1 can bind to Bcl-XL and is used in multi-target anticancer research.
    Caylin-1
  • 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-168226
    E3 ligase Ligand 34 2931870-73-2
    E3 ligase Ligand 34 is the E3 ligase ligand part of PROTAC SMARCA2/4-degrader-35 (HY-168225) and can be utilized in the synthesis of PROTACs.
    E3 ligase Ligand 34
  • 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-159973
    Me-SJ46411
    Me-SJ46411 is an E3 ubiquitin ligase ligand, which can be used for the synthesis of PROTAC molecules. For example, Me-SJ46411 combined with PROTAC linker Boc-Piperazine-OH (HY-20797) and target protein ligand (+)-JQ-1 (HY-13030) can be used to synthesize the selective BRD3 PROTAC degrader SJ46420 (HY-168635).
    Me-SJ46411
Cat. No. Product Name / Synonyms Application Reactivity
Ligands for E3 Ligase Isoform Comparison

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