Propargyl-PEG4-sulfonic acid
Propargyl-PEG4-sulfonic acid is a PEG-based linker bearing a terminal propargyl group for orthogonal conjugation and a sulfonic acid handle that provides strong aqueous solubility and ionic character. Structurally, it comprises a short, flexible polyethylene glycol chain that spaces functional termini to reduce steric interference and to support productive formation of ternary complexes in targeted protein degradation constructs. In PROTAC design, the propargyl functionality enables reliable bioorthogonal attachment (commonly via copper-catalyzed azide–alkyne cycloaddition or related click chemistries), allowing researchers to connect this linker to either the ligand or the E3-recruiting module through a stable triazole linkage. The sulfonic acid group can further improve handling in aqueous buffers and may help maintain solubility of the assembled degrader. This linker is valuable for constructing modular PROTACs where controlled spacing, conjugation flexibility, and experimental robustness are required for systematic structure–activity studies.
Structure of 1817735-29-7
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Propargyl-PEG4-sulfonic acid is a PEG-based linker building block designed for constructing PROTACs that require a flexible, water-compatible tether between a ligand and an E3 ligase-binding moiety. Its propargyl handle enables selective conjugation through well-established click-type coupling strategies, while the sulfonic acid functionality supports solubility and can help maintain productive linker behavior in aqueous media. The features and practical considerations for synthesis and PROTAC assembly are described in detail below.
Structure: The molecule combines a propargyl (alkyne) functional group with a poly(ethylene glycol) chain and a terminal sulfonic acid. It contains ether linkages within the PEG segment, a carbon–carbon triple bond at the propargyl site, and a strongly polar sulfonate group that enhances hydrophilicity and ionic character.
Reactivity: The terminal alkyne is suitable for copper-catalyzed azide–alkyne cycloaddition or related alkyne-based conjugation workflows commonly used in PROTAC synthesis. Typical assembly employs an appropriate Cu(I) source, a stabilizing ligand, and aqueous/organic mixed solvents to balance solubility of conjugates. Reaction performance is influenced by pH, oxygen sensitivity of Cu(I), and the presence of reactive functional groups on the partner ligands.
* 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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