DBCO-PEG4-PFP ester
Cat No.: BP-501900
Purity: 98%
4.5 
DBCO-PEG4-PFP ester is a heterobifunctional PEG-based linker combining a dibenzocyclooctyne (DBCO) handle for strain-promoted azide–alkyne cycloaddition (SPAAC) with a pentafluorophenyl (PFP) ester activated toward nucleophilic acyl substitution. Structurally, it features a short PEG4 spacer that provides aqueous solubility and spatial separation, while the PFP ester enables efficient conjugation to primary amines (e.g., lysine residues on proteins) or other nucleophiles under standard bioconjugation conditions. In PROTAC and targeted protein degradation workflows, this linker can be used to install a SPAAC-compatible tag on one component (such as a ligand or adaptor) and subsequently couple it to an azide-bearing partner, including E3-ligase ligands or handle-functionalized degraders, to assemble multicomponent constructs with controlled geometry. Its value lies in facilitating modular, catalyst-free conjugation and in improving conjugate handling and performance by reducing aggregation and steric constraints during degradation experiments.
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* For research and manufacturing use only. Not for human or clinical use.
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This DBCO-PEG4-PFP ester is a bifunctional PROTAC linker designed to connect a DBCO-based bioorthogonal handle to a PFP-activated ester for efficient coupling to amine-containing ligands. Its PEG spacer supports favorable solubility and enables controlled spatial presentation of the two functional regions, which can improve conjugation efficiency and accessibility in targeted protein degradation workflows. The detailed structural and reactivity considerations are provided below.
Structure: The linker combines a cyclooctyne (DBCO) moiety with a poly(ethylene glycol) spacer and a pentafluorophenyl (PFP) ester. It contains ether linkages within the PEG chain and an activated ester featuring an electron-poor aromatic leaving group, supporting selective acyl transfer chemistry under mild conditions.
Reactivity: The PFP ester undergoes nucleophilic acyl substitution with primary amines to form stable amide bonds, typically using aqueous or mixed aqueous buffers at controlled pH. The DBCO handle enables strain-promoted azide–alkyne cycloaddition with azide-bearing partners without added catalysts. For PROTAC assembly, amine coupling is performed first, followed by orthogonal click conjugation, using standard inert handling to 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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