Propargyl-PEG4-Sulfone-PEG4-acid
Propargyl-PEG4-Sulfone-PEG4-acid is a heterobifunctional polyethylene glycol (PEG) linker built from two PEG4 segments connected by a sulfone group, terminating in a propargyl (alkyne) handle and a carboxylic acid for further conjugation. The propargyl functionality enables chemoselective attachment through copper-free or copper-catalyzed azide–alkyne cycloaddition, making it suitable for modular PROTAC assembly where an E3 ligase ligand or targeting moiety can be “clicked” onto the linker. The carboxylic acid provides a reactive site for amide coupling to introduce the linker into carboxyl- or amine-bearing building blocks, while the sulfone and PEG chains improve aqueous solubility and conformational flexibility, helping maintain productive geometry for ternary complex formation. In targeted protein degradation research, this linker design supports systematic variation of spacing and attachment chemistry, facilitating optimization of degradation potency and selectivity while enabling reproducible synthesis of PROTAC candidates.
Structure of 2055024-41-2
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* For research and manufacturing use only. Not for human or clinical use.
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Propargyl-PEG4-Sulfone-PEG4-acid is a polyethylene glycol (PEG)-based PROTAC linker featuring a terminal alkyne handle and a sulfone-containing segment, coupled to a carboxylic acid for reliable conjugation chemistry. Its flexible, hydrophilic PEG architecture supports productive ternary-complex formation, while the sulfone motif can enhance linker polarity and stability. This product is designed for constructing targeted protein degraders, and the following points describe its structure and practical reactivity for PROTAC synthesis in detail.
Structure: The linker contains two PEG domains separated by a sulfone unit, providing conformational flexibility and increased polarity. A terminal propargyl (alkyne) group enables chemoselective coupling, while the carboxylic acid provides an anionic, hydrogen-bonding functionality. Ether linkages and sulfone connectivity dominate the framework.
Reactivity: The terminal alkyne is suitable for copper-catalyzed azide–alkyne cycloaddition or related click-type conjugations used in PROTAC assembly. The carboxylic acid is commonly activated for amide-bond formation via standard coupling strategies, enabling attachment to amine-bearing ligands. Reactions are typically performed under inert or controlled atmospheres with polar aprotic solvents, using appropriate catalysts or coupling reagents compatible with PEG and sulfone stability.
* 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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