Sulfone-Bis-PEG4-acid
Sulfone-Bis-PEG4-acid is a bifunctional PEG-based linker featuring a central sulfone core that connects two polyethylene glycol chains terminated with carboxylic acid groups. The PEG segments provide a hydrophilic, conformationally flexible spacer that can reduce steric interference between the two binding partners typically used in PROTAC constructs. In targeted protein degradation designs, this linker serves as a modular “bridge” that positions a ligand for an E3 ubiquitin ligase and a ligand for the target protein at an appropriate distance and orientation to promote formation of a productive ternary complex. The terminal acids enable straightforward conjugation to activated derivatives of ligands or to other linker fragments via amide or related coupling chemistries, facilitating systematic structure–activity optimization. This product is valuable for researchers seeking water-soluble, chemically versatile PROTAC linkers that can tune linker length and flexibility while maintaining compatibility with common synthetic workflows for targeted degradation studies.
Structure of 2055024-37-6
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* For research and manufacturing use only. Not for human or clinical use.
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Sulfonyl-based bis-PEG acid linker “Sulfone-Bis-PEG4-acid” is designed to provide a flexible, hydrophilic spacer for assembling PROTACs that rely on efficient ternary complex formation. Its PEG-rich architecture can improve aqueous solubility and help tune the effective distance and orientation between the target-binding ligand and the E3-recruiting moiety. The sulfone core adds chemical robustness, supporting reproducible linker behavior during synthesis and subsequent conjugation; detailed structural and reactivity considerations are provided below.
Structure: The linker features a central sulfone unit connected to two PEG chains terminating in carboxylic acid functionalities. Ether linkages within the PEG segments confer flexibility and strong hydrogen-bonding capacity, while the sulfone provides a polar, conformationally stabilizing motif. Overall, it is expected to be highly hydrophilic and compatible with aqueous PROTAC workflows.
Reactivity: The terminal carboxylic acids are suitable for standard PROTAC linker coupling via amide or related ester-forming chemistries. Typical approaches use carbodiimide-mediated activation (often with an auxiliary coupling reagent) to react with amine-containing ligands under mild, non-destructive conditions. Selection of polar aprotic solvents and careful pH control helps minimize PEG-related side reactions, while sulfone stability supports downstream handling during purification and characterization.
* 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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