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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.
(S)-Deoxy-thalidomide V97123 (S)-Deoxy-thalidomide 107657-57-8 (S)-Deoxythalidomide is an E3 ubiquitin ligase ligand.
(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,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,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.
(S,R,S)-AHPC-Ac V97362 (S,R,S)-AHPC-Ac 2361116-63-2 (S,R,S)-AHPC-Ac is a ligand for E3 ubiquitinases.
(S,R,S)-AHPC-acetyl-azetidine-PIP-boc V83764 (S,R,S)-AHPC-acetyl-azetidine-PIP-boc
(S,R,S)-AHPC-acetyl-Pip-O-azetidine-boc V83721 (S,R,S)-AHPC-acetyl-Pip-O-azetidine-boc
(S,R,S)-AHPC-Ala V97267 (S,R,S)-AHPC-Ala 2641319-58-4 (S,R,S)-AHPC-Ala is a ligand for E3 ubiquitinase.
(S,R,S)-AHPC-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH (VH032-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH) V82564 (S,R,S)-AHPC-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH (VH032-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH) 2086301-47-3 (S,R,S)-AHPC-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH (VH032-Boc-trans-3-aminocyclobutanol-Pip-CH2COOH) is a ligand (for E3 ligase)-linker conjugate ( E3 ligase ligand-linker conjugate), containing VHL ligand.
(S,R,S)-AHPC-C10-NHBoc V82555 (S,R,S)-AHPC-C10-NHBoc 2412055-13-9 (S,R,S)-AHPC-C10-NHBoc is a synthetic E3 ligase (e.g. CRBN) ligand-linker conjugate containing (S,R,S)-AHPC (HY -125845) VHL ligand and 1 linker.
(S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) V82542 (S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) 2597167-24-1 (S,R,S)-AHPC-C2-PEG4-N3 (VH032-C2-PEG4-N3) is a synthetic E3 ligase (e.g. CRBN) ligand-linker conjugate containing (S,R,S)- AHPC's VHL ligand and 4-unit PEG linker. (S,R,S)-AHPC-C2-PEG4-N3 may be utilized in the synthesis/preparation of vRucaparib-TP4 .
(S,R,S)-AHPC-CO-CH2-azetidine-piperazine-CH2-COOH V83795 (S,R,S)-AHPC-CO-CH2-azetidine-piperazine-CH2-COOH
(S,R,S)-AHPC-CO-CH2-O-CH2-piperidine-Boc V83777 (S,R,S)-AHPC-CO-CH2-O-CH2-piperidine-Boc
(S,R,S)-AHPC-CO-CH2-piperazine-C3-piperazine-Boc V83759 (S,R,S)-AHPC-CO-CH2-piperazine-C3-piperazine-Boc
(S,R,S)-AHPC-Me V2400 (S,R,S)-AHPC-Me 1948273-02-6 S,R,S)-AHPC-Me (also known as VHL ligand 2 or E3 ligase Ligand 1A) is the (S,R,S)-AHPC-based VHL ligand used in the recruitment of the von Hippel-Lindau (VHL) protein.
(S,R,S)-AHPC-O-CF3 V97277 (S,R,S)-AHPC-O-CF3 2641373-92-2 (S,R,S)-AHPC-O-CF3 is a ligand for E3 ubiquitinase.
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