Br-PEG2-THP
CAS No.: 152065-54-8
Cat No.: BP-500693
Purity: ≥95%
4.5 
Br-PEG2-THP is a bromine-terminated, short polyethylene glycol linker bearing a tetrahydropyran (THP) group, providing a chemically defined handle for PROTAC assembly and subsequent functionalization. The PEG2 segment offers aqueous compatibility and conformational flexibility, while the THP substituent can serve as a protected or modulated attachment motif depending on the synthetic strategy used to connect the two PROTAC ligands. In targeted protein degradation designs, such linkers are used to spatially separate the E3 ligase-binding moiety from the target-binding ligand, tuning effective ternary complex formation and degradation potency by controlling linker length, polarity, and local dynamics. The terminal bromide enables reliable coupling chemistries (e.g., nucleophilic substitution) to install the linker onto complementary functional groups, facilitating modular synthesis of PROTAC candidates. This product is therefore valuable for researchers optimizing linker architecture in structure–activity relationship studies, where small changes in linkage geometry and hydrophilicity can markedly affect cellular degradation outcomes.
Structure of 152065-54-8
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Br-PEG2-THP is a bromo-functional polyethylene glycol linker bearing a tetrahydropyran (THP) protected alcohol handle, designed to support modular PROTAC assembly. Its PEG segment provides conformational flexibility and improved solubility, while the bromo group enables efficient electrophilic coupling to nucleophilic partners. The THP protecting group offers a controlled functionalization strategy for stepwise synthesis. The detailed structural and reactivity characteristics are described below.
Structure: The linker comprises a PEG chain connected to a brominated terminus and a THP-protected oxygen functionality. It contains ether linkages along the PEG backbone and a cyclic acetal motif from THP, with a primary carbon–bromine bond at the reactive end. These features support solubility and orthogonal synthetic handling.
Reactivity: The bromo terminus is suitable for nucleophilic substitution reactions commonly used in PROTAC linker construction, where an appropriate nucleophile displaces bromide under base-assisted conditions. The THP group is typically stable to many coupling steps but can be removed under mild acidic conditions to reveal a free alcohol for subsequent ester or ether formation. Solvent systems are selected to balance nucleophile solubility and substitution efficiency, following standard ether/alkylation practices used in linker synthesis.
* 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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