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Ligands for E3 Ligase

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 transfer of ubiquitin and degradation of the targeted protein will occur as a result of the connection between an E3 ligase and a target protein brought on by a PROTAC.

E3 ligases determine the specificity of the proteins by catalyzing the transfer of ubiquitin to the desired proteins. Cells have hundreds of E3 ligases, but only a small number of them have been successfully exploited in PROTACs, including VHL (the tumor suppressor protein for von Hippel-Lindau disease), CRBN (Cereblon), MDM2 (the mouse double minute 2 homologue), and IAP (inhibitor of apoptosis).

Ligands for E3 Ligase related products

Structure Cat No. Product Name CAS No. Product Description
(3S)Lenalidomide-5-Br V97355 (3S)Lenalidomide-5-Br 2829898-76-0 (3S)Lenalidomide-5-Br is a ligand for E3 ubiquitinases.
(R)-Desamino lenalidomide-5-Br V113047 (R)-Desamino lenalidomide-5-Br 2243825-20-7 (R)-Deaminolenalidomide-5-Br is an E3 ubiquitin ligand that binds to cereblon (CRBN) protein and is used to recruit cereblon protein.
(R,R,R)-AHPC hydrochloride V112983 (R,R,R)-AHPC hydrochloride (R,R,R)-AHPC hydrochloride is an E3 ubiquitin ligand VHL used to recruit VHL proteins.
(R,R,S)-AHPC V113037 (R,R,S)-AHPC 2764746-08-7 (R,R,S)-AHPC ((R,R,S)-VH032-NH2) is a VHL ligand based on (S,R,S)-AHPC that recruits the von Hippel-Lindau (VHL) protein.
(R,S,R)-AHPC-Me-Ac V120143 (R,S,R)-AHPC-Me-Ac (R,S,R)-AHPC-Me-Ac is an E3 ligase ligand that can be used to synthesize PROTAC SHP2 protein degrader-2.
(R,S,R)-AHPC-NHBoc V112927 (R,S,R)-AHPC-NHBoc 1799506-31-2 (R,S,R)-AHPC-NHBoc is an E3 ubiquitin ligand and also a VHL ligand used to recruit VHL proteins.
(R,S,S)-VH032-Me TFA V120123 (R,S,S)-VH032-Me TFA 2451573-93-4 (R,S,S)-VH032-Me TFA is an E3 ligase ligand that can be used to synthesize dTAGV-1 hydrochloride.
(rel)-Nutlin carboxylic acid V111867 (rel)-Nutlin carboxylic acid 2760669-71-2 (rel)-Nutlin carboxylic acid is an MDM2 ligand based on Nutlin 3.
(S)-(S,R,S,R)-AHPC-Me-N3 V104992 (S)-(S,R,S,R)-AHPC-Me-N3 2958620-43-2 (S)-(S,R,S,R)-AHPC-Me-N3 is the E3 ligase ligand of PROTAC SMARCA2 degrader-32 and can be used for the synthesis of PROTAC.
(S)-Deoxy-thalidomide V97123 (S)-Deoxy-thalidomide 107657-57-8 (S)-Deoxythalidomide is an E3 ubiquitin ligase ligand.
(S)-Deoxy-thalidomide-Br V104287 (S)-Deoxy-thalidomide-Br (S)-Deoxythalidomide-Br is a ligand for the E3 ligase and was used to synthesize PROTAC FHD-609.
(S)-PROTAC PTK6 ligand-1-(2S,4R)-O-CH2-O-hygric acid V83803 (S)-PROTAC PTK6 ligand-1-(2S,4R)-O-CH2-O-hygric acid
(S)-PROTAC PTK6 ligand-O-4,4-dimethylpiperidine-Boc V83735 (S)-PROTAC PTK6 ligand-O-4,4-dimethylpiperidine-Boc
(S)-PROTAC PTK6 ligand-O-C2-O-piperidine-Boc V83726 (S)-PROTAC PTK6 ligand-O-C2-O-piperidine-Boc
(S)-Thalidomide-5-OH V112556 (S)-Thalidomide-5-OH 172333-29-8 (S)-Thalidomide-5-OH is the E3 ubiquitin ligand for cereblon (CRBN) protein, used to recruit cereblon protein.
(S,R,R)-VH032 V100321 (S,R,R)-VH032 2489876-59-5 (S,R,R)-VH032 (compound V3) is a VHL ligand that can be used to synthesize PROTAC NCOA4 degrader-1.
(S,R,R)-VH032 hydrochloride V113722 (S,R,R)-VH032 hydrochloride 2761478-98-0 (S,R,R)-VH032 hydrochloride is a VH032-based VHL ligand that recruits the von Hippel-Lindau (VHL) protein.
(S,R,S)-AHPC 2-OH hydrochloride V113717 (S,R,S)-AHPC 2-OH hydrochloride 2244684-41-9 (S,R,S)-AHPC 2-OH hydrochloride is an E3 ubiquitin ligand that can be used to recruit VHL proteins.
(S,R,S)-AHPC dihydrochloride (VH032-NH2 dihydrochloride; VHL ligand 1 dihydrochloride) V85210 (S,R,S)-AHPC dihydrochloride (VH032-NH2 dihydrochloride; VHL ligand 1 dihydrochloride) 2137142-47-1
(S,R,S)-AHPC(Me)-amido-C2-acid V89049 (S,R,S)-AHPC(Me)-amido-C2-acid 2365173-01-7 (S,R,S)-AHPC(Me)-amido-C2-acid is a VHL (E3 ligase) ligand that can be used to synthesize PROTACs, such as PROTAC STING Degrader-2.
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