Br-PEG4-THP
Br-PEG4-THP is a bromine-terminated, tetraethylene glycol–based polyethylene glycol (PEG) linker bearing a tetrahydropyran (THP) ether functionality. Structurally, it provides a flexible, hydrophilic spacer of short PEG chain length coupled through an ether linkage to a THP-protected alcohol motif, enabling controlled presentation of reactive handles for PROTAC assembly. In targeted protein degradation designs, such linkers are used to tune the effective distance and relative orientation between the ligand-binding moieties (e.g., E3 ligase binder and target binder), thereby optimizing formation of the ternary complex and improving degradation efficiency. The bromine terminus serves as a chemically addressable site for subsequent conjugation or substitution reactions, while the THP group can support synthetic strategies that protect or modulate alcohol reactivity during linker construction. This reagent is valuable for researchers seeking modular, reproducible linker synthesis to systematically evaluate how spacer length and polarity influence PROTAC performance.
Structure of 1803547-60-5
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Br-PEG4-THP is a bromo-terminated polyethylene glycol (PEG) linker designed for efficient conjugation in targeted protein degradation (PROTAC) workflows. Its PEG-based spacer supports productive ternary complex formation by improving solubility and conformational flexibility, while the bromide handle enables reliable attachment to partner ligands. The following sections describe the linker’s structure and the practical reactivity considerations for PROTAC assembly.
Structure: The molecule combines a PEG chain with a terminal bromide electrophile and a THP (tetrahydropyran) motif, providing an ether-rich, flexible scaffold. It contains C–Br and ether (C–O–C) linkages, with polarity that enhances aqueous compatibility and supports stable linker behavior during bioconjugation.
Reactivity: The bromide functionality is suited to nucleophilic substitution or related coupling strategies commonly used to connect PROTAC components. Linker installation is typically performed under conditions that maintain electrophile reactivity while preserving ligand integrity, using polar aprotic solvents or compatible mixed solvents. Reaction design should account for PEG-mediated solvation effects and, where relevant, THP stability under the chosen base or nucleophile.
* 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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