Tos-PEG6-THP
CAS No.: 669556-37-0
Cat No.: BP-500889
Purity: ≥95%
4.5 
Tos-PEG6-THP is a heterobifunctional PROTAC linker built on a polyethylene glycol chain of six ethylene glycol units, terminating in a tosyl-activated group and a tetrahydropyran (THP) functionality. The tosyl group provides a robust leaving group for nucleophilic substitution, enabling controlled conjugation to amine- or thiol-containing handles on a targeting ligand or E3 ligase binder, while the PEG segment imparts aqueous solubility, conformational flexibility, and reduced steric interference between the two recruited binding domains. In targeted protein degradation workflows, such linkers are used to position the two pharmacophores at an appropriate effective distance and orientation to promote formation of a productive ternary complex and subsequent ubiquitination-driven degradation. This linker is valuable for researchers optimizing PROTAC efficacy and selectivity, particularly when tuning linker length and polarity to balance binding, cell permeability, and degradation potency.
Structure of 669556-37-0
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Tos-PEG6-THP is a PEG-based linker reagent designed to support efficient conjugation in PROTAC architectures, enabling controlled spatial separation between the ligand moieties and tuning of physicochemical properties such as solubility and conformational flexibility. Its ether-rich PEG segment can reduce steric constraints at the ternary-complex interface, which is often beneficial for targeted protein degradation workflows. The following sections describe the linker’s structural features and practical reactivity considerations for PROTAC assembly in the laboratory.
Structure: Tos-PEG6-THP comprises a tosyl-protected PEG chain linked to a tetrahydropyranyl (THP) ether functionality. It contains ether linkages and an aromatic sulfonyl group, providing a polar, flexible scaffold with stable covalent connectivity under typical organic synthesis conditions.
Reactivity: Tosyl-activated PEG linkers are commonly used in PROTAC synthesis via nucleophilic substitution or related coupling steps, where the sulfonate activation facilitates displacement by appropriate nucleophiles. THP ethers can be selectively deprotected under mild, acid-mediated conditions to reveal alcohol functionality for subsequent bond formation. Choice of solvent and base should be aligned with the nucleophile and protecting-group stability to preserve the PEG backbone during assembly.
* 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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