benzyl peg4 amine

Benzyl-PEG4-amine, a PEG-based linker for PROTACs, connects two essential ligands necessary for forming PROTAC molecules, facilitating selective protein degradation via the ubiquitin-proteasome system within cells.

Boc-PEG4-Val-Cit-PAB-OH is an enzyme-cleavable ADC linker that features a Boc-protected amine, a hydrophilic PEG spacer, and a Val-Cit-PAB dipeptide. The benzyl alcohol on PAB is useful for attaching reactive groups (e.g., PNP) to bind with drug payloads. Acidic conditions can remove the Boc protecting group, exposing the primary amine for conjugation reactions to form amides. The Val-Cit-PAB segment can be cleaved by intracellular proteases, allowing efficient payload release within cells.

Fmoc-PEG4-Val-Cit-PAB-OH is an enzyme-cleavable ADC linker that incorporates a Boc-protected amine, a hydrophilic PEG spacer, and a Val-Cit-PAB dipeptide. The benzyl alcohol on PAB can be used to attach reactive groups (such as PNP) for drug payload conjugation. The Fmoc protecting group can be removed with piperidine to expose a primary amine, facilitating amide bond formation. Val-Cit-PAB is cleaved by cellular proteases to efficiently release the payload inside cells.

NH2-PEG4-Val-Cit-PAB-OH is a cleavable ADC linker that features a primary amine, a hydrophilic PEG spacer, a Val-Cit dipeptide, and a PAB group. The benzyl alcohol on the PAB component is suitable for attaching reactive groups (such as PNP) to facilitate binding with drug payloads. The primary amine is versatile for reactions such as coupling with carboxylic acids, reductive amination with ketones or aldehydes, or other specialized applications like SNAr reactions or heterocyclic chemistry. The Val-Cit dipeptide is cleaved by intracellular cathepsins, allowing efficient payload delivery via an elimination mechanism through the PAB structure.