PEG

Pomalidomide-amido-C3-COOH is a PROTAC linker featuring a pomalidomide, a pentyl spacer, and a carboxylic acid. Pomalidomide recruits E3 ligase for the ubiquitinylation and subsequent proteolysis of a given protein. Meanwhile, the carboxylic acid may react with amines in the presence of coupling reagents such as EDC or HATU.

Thalidomide-NH-C6-NH-Boc is a PROTAC linker featuring a thalidomide, a hydrophilic PEG spacer, and a Boc-protected amine. Thalidomide is an E3 ligase activator, promoting the ubiquitinylation of a given protein. Meanwhile, the Boc protecting group may be removed to reveal a primary amine which reacts with a variety of substrates.

CP-10 is a PROTAC molecule composed of ligands targeting Cereblon and CDK. It exhibits highly selective and specific degradation of CDK6, with a DC50 of 2.1 nM. CP-10 is potent in degrading both mutated and overexpressed CDK6, making it a valuable tool in PROTAC development.

5-Hydroxy-2-(1-methyl-2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione is a thalidomide analogue featuring a hydroxy group, which is a versatile site for further derivitization. Thalidomide is an E3 ligase activator and promotes the ubiquitinylation of a given protein.

2-(2,6-dioxopiperidin-3-yl)-4-({2-[2-(2-hydroxyethoxy)ethoxy]ethyl}amino)-2,3-dihydro-1H-isoindole-1,3-dione is a PROTAC linker featuring a thalidomide, a hydrophilic PEG spacer, and an alcohol. Thalidomide is an E3 ligase activator, promoting the proteolysis of a given protein. Meanwhile, the alcohol group is a versatile site for further derivitization.

2-Chloro-N-(2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)acetamide is a thalidomide analogue. Thalidomide recruits E3 Ligase for the ubiquitinylation and subsequent destruction of a given protein. This structure features a chloroacetamide, which is a thiol-specific reactive group.

tert-Butyl 2-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)acetate is a PROTAC linker featuring a thalidomide analogue, a hydrophilic PEG spacer, and a t-butyl ester. Thalidomide recruits E3 Ligase for the ubiquitinylation and subsequent destruction of a given protein. Meanwhile, the t-butyl ester can be hydrolyzed to reveal a carboxylic acid for further derivitization.

Thalidomide-NH-PEG4-COOH is a PROTAC linker featuring a thalidomide, a hydrophilic PEG spacer, and a carboxylic acid. Thalidomide recruits E3 Ligase for the ubiquitinylation and subsequent destruction of a given protein. The carboxylic acid is reactive towards amines and alcohols with the use of coupling reagents such as EDC or HATU.

2-(2,6-Dioxopiperidin-3-yl)-4-methylisoindoline-1,3-dione is an E3 ligase activator featuring a methyl group. E3 ligase is a protein that marks other proteins for proteolytic destruction by labeling them with ubiquitin.