PEG

2,3,4-(PEG4-Azide)-1-(PEG4-N-Boc)methane is a multifunctional PEG linker containing three azides and a Boc-protected primary amine. Azides are commonly used reagents in click chemistry, easily reacting with terminal alkynes or strained cyclooctynes like BCN or DBCO to form stable triazole links with the target molecule. The primary amine can be used for coupling to carboxylic acids in the presence of an activator such as EDC or HATU to form amide bonds.

2,3-(PEG4-Azide)-1-(PEG4-N-Boc)methane is a trifunctional PEG compound containing two azides and a Boc-protected primary amine. Azides are highly reactive towards terminal alkynes and strained cyclooctynes such as DBCO and BCN, while the amine may be deprotected under acidic conditions to allow for nucleophilic activity, such as in forming amides from carboxylic acids.

N-[2-(2,6-Dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl]-b-alanine is an E3 ligase activator featuring a carboxylic acid, which is reactive towards amines and alcohols in the presence of coupling reagents.

Thalidomide-NH-C2-PEG3-OH is a PROTAC linker featuring a thalidomide, a hydrophilic PEG spacer, and an alcohol. Thalidomide is an E3 ligase activator, promoting the ubiquitinylation of a given protein. Meanwhile, the hydroxyl is a versatile group which may react in a number of ways.

Thalidomide-O-amido-C3-PEG3-C1-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporatess the Thalidomide based cereblon ligand and 3-unit PEG linker used in PROTAC technology.

Pomalidomide-C2-amido-(C1-O-C5-O-C1)2-COOH is a PROTAC linker featuring a pomalidomide, a hydrophilic PEG spacer, and a carboxylic acid. Pomalidomide is an E3 ligase activator, and this structure may be further derivatized via its carboxylic acid.

5-(Bromomethyl)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione is an E3 ligase activator which may be further derivatized by substitution at bromide.

Thalidomide-NH-PEG2-COOH is a PROTAC linker featuring a thalidomide, a hydrophilic PEG spacer, and a carboxylic acid. Thalidomide is an E3 ligase activator, promoting the ubiquitinylation of a given protein. Meanwhile, the carboxylic acid may react with amines in the presence of coupling reagents.

Thalidomide-O-C8-Boc is a PROTAC linker featuring a thalidomide, a hydrophilic PEG spacer, and a t-butyl ester. Thalidomide is an E3 ligase activator, promoting the ubiquitinylation of a given protein. Meanwhile, the t-butyl ester can be hydrolyzed to reveal a carboxylic acid for further derivatization.