Ald-PEG1-C2-Boc
Ald-PEG1-C2-Boc is a bifunctional, PEG-based PROTAC linker bearing an aldehyde handle and a tert-butyl ester-protected carboxylic acid, connected through a short ethylene (C2) spacer. The PEG1 segment provides aqueous solubility and conformational flexibility, while the aldehyde enables chemoselective conjugation strategies such as reductive amination or formation of reversible adducts with primary amines on targeting ligands or other PROTAC modules. The tert-butyl ester can be removed to reveal a carboxylic acid for subsequent activation and coupling, allowing stepwise assembly of multi-component degraders. In PROTAC design, such linkers help position the E3 ligase-binding moiety and the target-binding ligand at an appropriate distance and geometry, improving productive ternary-complex formation and thereby influencing degradation potency and selectivity. This linker is therefore valuable for rapid, modular synthesis and optimization of targeted protein degradation constructs.
Structure of 2100306-48-5
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* For research and manufacturing use only. Not for human or clinical use.
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Ald-PEG1-C2-Boc is a functionalized polyethylene glycol-based PROTAC linker designed to connect a ligand-bearing aldehyde handle to amine-bearing partners while incorporating a tert-butyl ester-protected carboxylic acid for controlled downstream coupling. Its PEG segment supports favorable solubility and linker flexibility, which can improve productive ternary complex formation in targeted protein degradation workflows. The structure and reactivity considerations for assembling PROTACs with this linker are described in detail below.
Structure: The linker comprises an aldehyde-functional group, a short ethylene spacer, and a PEG segment, together with a tert-butyl ester-protected carboxylic acid. It contains ether linkages within the PEG domain and an aldehyde carbonyl, together with an acid-labile tert-butyl ester for orthogonal reactivity under mild conditions.
Reactivity: The aldehyde can undergo chemoselective coupling with primary amines via reductive amination to form a stable secondary amine linkage. The tert-butyl ester enables protection during earlier steps and can be removed under standard acid-mediated deprotection to reveal a carboxylic acid for subsequent conjugation. Typical conditions use compatible alcohol or amine solvents and reducing agents appropriate for reductive amination, with careful control of pH to preserve Boc integrity when required.
* 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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