Azido-PEG3-Sulfone-PEG4-Boc
CAS No.: 2055023-76-0
Cat No.: BP-501596
Purity: 97%
4.5 
Azido-PEG3-Sulfone-PEG4-Boc is a heterobifunctional, PEG-based PROTAC linker featuring an azide handle for bioorthogonal conjugation, a sulfone-containing segment that provides a chemically robust, polar connection, and terminal Boc protection that enables controlled coupling chemistry during linker assembly. Structurally, it comprises short polyethylene glycol chains separated by a sulfone linkage, yielding a flexible, water-compatible scaffold with defined attachment points for installing a ligand warhead and an E3-recruiting moiety. In PROTAC design, the azide group can be used for azide–alkyne cycloaddition or related click-type strategies to connect the linker to complementary partners, while the sulfone and PEG segments help tune solubility, reduce nonspecific hydrophobic interactions, and maintain productive spatial orientation between the two binding domains. This linker is valuable for constructing targeted protein degraders where modular synthesis, aqueous handling, and reliable conjugation are required to generate well-defined, tunable degraders for mechanistic and structure–activity studies.
Structure of 2055023-76-0
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This azido-functional PEG-based linker is designed for constructing PROTACs that require efficient, modular conjugation to targeting ligands while maintaining favorable solubility and conformational flexibility. Its PEG-rich architecture provides hydrophilic spacing for targeted protein degradation conjugation workflows. The azide handle enables orthogonal bioorthogonal coupling strategies, and the sulfone-containing segment provides a stable, chemically robust scaffold. Detailed structural and reactivity considerations are provided below.
Structure: The linker comprises polyethylene glycol segments connected through a sulfone-containing linkage and terminated with a tert-butyl ester-protected carboxyl group, alongside a terminal azide. It features ether-rich PEG chains, a sulfone (S(=O)2) moiety, and an azide for click-type chemistry. Overall, it is expected to be flexible and polar, supporting aqueous compatibility.
Reactivity: The azide group is suitable for copper-catalyzed azide–alkyne cycloaddition or related azide-based conjugation approaches, typically performed in polar organic/aqueous mixtures under conditions that preserve sensitive PROTAC ligands. The sulfone and PEG framework are generally stable to standard coupling conditions. The tert-butyl ester can be cleaved using established acid-mediated conditions to reveal the carboxylic acid for subsequent activation and coupling, often without disrupting PEG integrity.
* 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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