PEG

N-Boc-N-bis(PEG8-alcohol) is a bifunctional linker with two primary alcohols linked by a Boc-protected secondary amine. The alcohols can be used in a number of ways such as for creating esters with carboxylic acids, while the secondary amine can be deprotected and for subsequent reactions with carboxylic acids, ketones, or aldehydes.

N-Boc-N-bis(PEG8-alcohol) is a bifunctional linker with two primary alcohols linked by a Boc-protected secondary amine. The alcohols can be used in a number of ways such as for creating esters with carboxylic acids, while the secondary amine can be deprotected and for subsequent reactions with carboxylic acids, ketones, or aldehydes.

N-Mal-N-bis(PEG8-acid) is a trifunctional linker with two carboxylic acids and a maleimide group. The carboxylic acids can react with primary amines in the presence of a coupling reagent such as HATU or EDC to form stable amide bonds. Maleimide is a covalent ligand used for linking thiols such as those in cysteines residues in proteins. The PEG spacers make this molecule water-soluble, potentially altering its DMPK properties.

N-(NH-Boc-PEG4)-N-bis(PEG4-azide) is a trifunctional linker containing two azides and a Boc-protected primary amine. The azide group is reactive towards terminal alkynes and strained cyclooctynes using click chemistry. The Boc can be removed using acidic conditions to allow the amine to react with carboxylic acids to form stable amide bonds. PEG linkers provide high aqueous solubility, and altering PEG length can alter DMPK.

HO-PEG-Succinimidyl Carbonate, MW 2,000 is a PEG linker containing a succinimidyl carbonate and an alcohol group. The succinimidyl carbonate is a good leaving group that is easily substituted by nucleophiles under mild conditions while the alcohol is a versatile building block that can be applied in a number of ways such as forming esters, ethers, carbonyls and so on.

N-(Azide-PEG8-carbonyl)-N-bis(PEG8-t-butyl ester) is a trifunctional reagent with two t-butyl ester and an azide. The azide group can be used to label terminal alkynes and strained cyclooctynes like BCN or DBCO using click chemistry. The t-butyl esters can be deprotected using acid or base to allow for attack from amines or alcohols. The central junction is a tertiary amide, allowing for hydrogen bonding effects to increase this molecule’s aqueous solubility.

Propargyl-PEG2-NHS ester is a PEG linker with a propargyl group that can participate in copper catalyzed azide-alkyne Click Chemistry and NHS ester that can be used to label amine-containing entitites.

N-(DBCO)-N-bis(PEG4-Amine) is a trifunctional reagent with two primary amines and a DBCO moiety annealed to a central tertiary amine. The DBCO is a strained cyclooctyne, perfect for labeling azide residues on a target molecule using click chemistry, while the primary amines can be used for reactions with carboxylic acids, aldehydes, or ketones.

Thalidomide-5-(PEG2-Azide) is a PROTAC linker featuring a thalidomide ligand connected to a PEG spacer and an azide group. Azides are click chemistry handles that are capable of reacting with terminal alkynes or strained cyclooctynes. Thalidomide is a ligand for E3 ligase, which ubiquitinylates proteins, thus committing their fate to proteolytic destruction.