DBC0-NH-PEG4-amine is a bifunctional, PEG-based linker featuring a dibenzocyclooctyne (DBCO) group for strain-promoted azide–alkyne cycloaddition (SPAAC) and a terminal primary amine for covalent coupling to amine-reactive or activated carboxyl/activated ester chemistries. The PEG4 spacer provides a flexible, hydrophilic chain that helps reduce steric hindrance and improves the accessibility of the reactive handles, enabling efficient conjugation under copper-free conditions that are commonly preferred for sensitive biological systems. In PROTAC and targeted protein degradation workflows, this linker can be used to attach one PROTAC module (e.g., an E3 ligase ligand or a targeting moiety) to an azide-functional partner, forming a stable triazole linkage via SPAAC, while the amine handle supports alternative attachment strategies such as amide bond formation. Its modular reactivity and biocompatible conjugation profile make it valuable for assembling degraders, optimizing linker length/geometry, and generating structure–activity relationship libraries.
Structure of 1255942-08-5
* For research and manufacturing use only. Not for human or clinical use.
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This DBCO-NH-PEG4-amine linker is designed for modular construction of PROTACs and related targeted protein degradation conjugates by enabling efficient, chemoselective attachment to biomolecules. Its DBCO handle supports rapid strain-promoted azide–alkyne cycloaddition, while the PEG-based chain provides solubility and conformational flexibility that can improve conjugation performance and linker presentation. Detailed structural and reactivity considerations are provided below.
Structure: The linker contains a dibenzocyclooctyne (DBCO) moiety connected through an amide to a polyethylene glycol (PEG) segment terminating in a primary amine. It features an alkynyl cyclooctyne for SPAAC and amide and ether linkages that confer hydrophilicity, flexibility, and stable covalent connectivity for PROTAC assembly.
Reactivity: The DBCO group reacts with azide-functional partners via strain-promoted azide–alkyne cycloaddition under catalyst-free conditions, typically in aqueous-compatible buffers. The terminal amine enables standard amide- or urea-forming coupling strategies with activated carboxylic acids or isocyanates, allowing installation of the linker into PROTAC architectures. Use of mild, non-nucleophilic conditions helps preserve azide/alkyne reactivity and minimize side reactions.
* 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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