N-(Hydroxy-PEG3)-N-Boc-PEG4-Boc
N-(Hydroxy-PEG3)-N-Boc-PEG4-Boc is a heterobifunctional polyethylene glycol (PEG) linker featuring a terminal hydroxy group, an N-Boc-protected amine, and a tert-butyl ester-protected carboxyl group, with PEG3 and PEG4 segments around the central nitrogen. The hydroxy terminus provides a convenient handle for controlled coupling to electrophilic groups (e.g., activated esters or carbonyl derivatives), while the N-Boc group masks the amine and the tert-butyl ester protects the carboxyl group to reduce nonspecific reactivity during PROTAC assembly. Upon appropriate deprotection, the liberated amine and/or carboxylic acid can be used for amide or urea-forming coupling strategies, enabling stepwise conjugation of a ligand-binding warhead to a second component such as an E3 ligase recruiter. In targeted protein degradation research, PEG-based linkers like this can improve aqueous compatibility, tune linker flexibility and effective distance between binding domains, and thereby support robust ternary complex formation and degradation efficiency.
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* For research and manufacturing use only. Not for human or clinical use.
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This PROTAC linker component is designed to provide a tunable, hydrophilic polyethylene glycol (PEG)-based spacer architecture that can improve solubility and modulate the effective reach between a target-binding ligand and an E3 ligase ligand. Its protected functional groups enable controlled synthetic elaboration during PROTAC assembly, supporting modular linker installation and subsequent deprotection/functionalization steps. Detailed structural and reactivity considerations are provided below for experimental planning.
Structure: The molecule contains PEG oligomer segments bearing a terminal hydroxyl group, one Boc-protected amine, and one tert-butyl ester-protected carboxyl group. It features ether linkages characteristic of PEG, one Boc carbamate, and one tert-butyl ester, offering flexibility, polarity, and orthogonal protection under standard organic synthesis conditions.
Reactivity: The Boc-protected amine and tert-butyl ester-protected carboxyl group can be carried through compatible non-acidic coupling and linker-functionalization steps. Acid-mediated deprotection can reveal the amine from the Boc carbamate and the carboxylic acid from the tert-butyl ester; subsequent coupling should be selected according to the functional handle required. PEG ether backbones generally tolerate common organic solvents used in peptide-ligand coupling workflows.
* Our calculator is based on the following equation:
Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
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