DBCO-C2-PEG4-amine
DBCO-C2-PEG4-amine is a bifunctional, PEG-based linker bearing a dibenzocyclooctyne (DBCO) moiety and a terminal primary amine, connected through a short ethylene (C2) spacer and a four-unit poly(ethylene glycol) chain. Structurally, it combines a strain-promoted alkyne handle for copper-free azide–alkyne cycloaddition with an amine group that enables straightforward conjugation to activated carboxylates, isothiocyanates, or other electrophiles used to attach PROTAC warheads or targeting ligands. In PROTAC design, this linker is used to spatially tune the distance and flexibility between the two functional components, improving productive formation of the ternary complex by allowing favorable orientation and reducing steric clashes. Its PEG segment also enhances aqueous solubility and can mitigate aggregation during synthesis and biological assays. Overall, it is a practical reagent for modular assembly of targeted protein degraders, facilitating rapid, site-specific coupling under mild conditions.
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* For research and manufacturing use only. Not for human or clinical use.
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DBCO-C2-PEG4-amine is a bifunctional, PEG-based linker designed to support modular PROTAC construction by enabling efficient conjugation to azide-bearing targeting ligands and to complementary handles used for assembling ternary degradation platforms. Its flexible poly(ethylene glycol) segment can improve solubility and reduce steric constraints around the conjugation site, supporting robust formation of productive linker–ligand architectures. The points below describe its structure and practical reactivity for experimental PROTAC synthesis.
Structure: The linker contains a DBCO cyclooctyne moiety connected through a short carbon spacer to a PEG chain terminating in a primary amine. It features ether linkages within the PEG segment, an alkyne-containing strained ring for click reactivity, and a reactive amine for further derivatization.
Reactivity: DBCO groups undergo strain-promoted azide–alkyne cycloaddition with azides under mild, catalyst-free conditions, typically in aqueous or mixed aqueous/organic media compatible with biomolecule conjugation. The terminal primary amine enables standard amide or urea coupling strategies using activated carboxylic acids or isocyanates, allowing attachment to protein-binding ligands or further PROTAC components. Reaction design should consider solvent compatibility and maintaining azide/DBCO integrity during assembly.
* 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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