Hydroxy-PEG10-CH2-Boc
Hydroxy-PEG10-CH2-Boc is a PEG-based linker featuring a terminal hydroxyl group and a methylene handle for attachment, together with a tert-butyl ester-protected carboxyl group that can be deprotected under acidic conditions to reveal a carboxylic acid for subsequent conjugation. The PEG chain provides a flexible, hydrophilic spacer that can reduce steric interference between the two binding modules of a PROTAC, helping maintain productive geometry for ternary complex formation. In targeted protein degradation workflows, this type of linker is commonly used to connect a ligand for an E3 ubiquitin ligase to a ligand or binding moiety for the target protein, thereby enabling ubiquitination and proteasomal degradation when the conjugate brings the proteins into proximity. Its ether-rich backbone can improve solubility and facilitate synthesis of modular degraders, making it a practical building block for systematic linker-length and attachment-position optimization in structure–activity relationship studies.
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* For research and manufacturing use only. Not for human or clinical use.
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This Hydroxy-PEG10-CH2-Boc linker is a polyethylene glycol-based, Boc-protected functional spacer designed to support modular PROTAC assembly. Its ether-rich PEG backbone provides conformational flexibility and improved solubility, while the terminal hydroxyl and protected amine handle enable controlled conjugation to targeting ligands and E3-recruiting moieties. The linker’s design facilitates efficient synthesis of degraders and allows tuning of linker length and attachment chemistry; detailed structural and reactivity considerations are provided below.
Structure: The linker contains a PEG chain with multiple ether linkages, providing a hydrophilic, flexible scaffold. A terminal hydroxymethyl group supports hydrogen-bonding and solvation, while a Boc-protected functionality offers chemical stability during coupling steps. Overall, it behaves as a polar, ether-containing spacer.
Reactivity: The Boc group can be removed under standard acidolysis conditions to reveal the reactive amine for subsequent amide or carbamate-forming couplings. Conjugation to PROTAC warheads is typically achieved via amide coupling using activated carboxylic acids or via carbamate formation from hydroxyl-bearing intermediates. Commonly used catalysts include coupling reagents for amide bond formation, with polar aprotic solvents and controlled temperature to maintain linker integrity.
* 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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