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PROTAC-E3 Ligase Ligands

Bifunctional degrader molecules, also called proteolysis-targeting chimeras (PROTACs), are a new modality of chemical tools and potential therapeutics to understand and treat human disease. A required PROTAC component is a ligand binding to an E3 ubiquitin ligase, which is then joined to another ligand binding to a protein to be degraded via the ubiquitin–proteasome system. The advent of nonpeptidic small-molecule E3 ligase ligands revolutionized the field and ushered in the design of drug-like PROTACs with potent and selective degradation activity.

3-(4-amino-1-oxoisoindolin-2-yl)piperidine-2,6-dione hemihydrate

3-[6-(aminomethyl)-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione

3-[7-(aminomethyl)-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione

2-(2,6-dioxopiperidin-3-yl)-4-hydroxyisoindole-1,3-dione

2-(2,6-Dioxopiperidin-3-yl)-5-hydroxyisoindoline-1,3-dione

(2S,4R)-1-[(2S)-2-acetamido-3,3-dimethylbutanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide

3-(6-bromo-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione

3-(7-hydroxy-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione

2-(2,6-dioxopiperidin-3-yl)-4-fluoroisoindole-1,3-dione

2-(2,6-dioxopiperidin-3-yl)-5-fluoroisoindole-1,3-dione

2-(2,6-dioxopiperidin-3-yl)-4-prop-2-ynoxyisoindole-1,3-dione

3-(6-hydroxy-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione

2,6-Piperidinedione, 3-(6-fluoro-1,3-dihydro-1-oxo-2H-isoindol-2-yl)-

3-[6-(aminomethyl)-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione;hydrochloride

(2S,4R)-1-[(2S)-3,3-dimethyl-2-[(2-prop-2-ynoxyacetyl)amino]butanoyl]-4-hydroxy-N-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methyl]pyrrolidine-2-carboxamide

L-Leucine, N-[(2S,3R)-3-[[(9H-fluoren-9-ylmethoxy)carbonyl]amino]-2-hydroxy-1-oxo-4-phenylbutyl]-

Acetic acid, 2-[[1-(2-chloroacetyl)-1,2,3,4-tetrahydro-6-quinolinyl]oxy]-

Nonanoic acid, 9-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]-, 1,1-dimethylethyl ester

3-(7-amino-3-oxo-1H-isoindol-2-yl)piperidine-2,6-dione;hydrochloride

Acetaldehyde, 2-[2-[2-[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]amino]ethoxy]ethoxy]ethoxy]-

2-[4-[(4R,5S)-4,5-bis(4-chlorophenyl)-2-(4-methoxy-2-propan-2-yloxyphenyl)-4,5-dihydroimidazole-1-carbonyl]-2-oxopiperazin-1-yl]acetic acid

(2S)-2-[[(2S,3R)-2-hydroxy-3-[(2-methylpropan-2-yl)oxycarbonylamino]-4-phenylbutanoyl]amino]-4-methylpentanoic acid

4,5,6,7-tetradeuterio-2-(2,6-dioxopiperidin-3-yl)isoindole-1,3-dione

3-[7-(aminomethyl)-3-oxo-1H-isoindol-2-yl]piperidine-2,6-dione;hydrochloride