Propargyl-PEG5-PFP ester
CAS No.: 2148295-92-3
Cat No.: BP-501306
4.5 
Propargyl-PEG5-PFP ester is a heterobifunctional PEG-based linker combining a terminal propargyl group with a pentaglycol (PEG5) spacer and a pentafluorophenyl (PFP) ester reactive toward nucleophilic amines, including lysine residues on proteins and primary amine handles on small-molecule ligands. Structurally, it provides a flexible hydrophilic chain that helps control conjugation distance and reduces steric interference, while the PFP ester enables efficient coupling under conditions commonly used for amide-bond formation. In PROTAC and targeted degradation workflows, this linker is used to install a defined attachment point on one component (e.g., a ligand or E3-recruiting moiety) via amide formation, and the propargyl group can subsequently participate in copper-catalyzed azide–alkyne cycloaddition (CuAAC) for orthogonal “click” assembly with a second partner. Its value lies in enabling modular synthesis, improving solubility, and supporting reproducible construction of degraders for mechanistic and optimization studies.
Structure of 2148295-92-3
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Propargyl-PEG5-PFP ester is a PEG-based, bifunctional linker designed for efficient assembly of PROTAC constructs, combining a terminal alkyne handle with a PFP ester for selective amide formation. Its PEG segment promotes aqueous compatibility and can enhance effective conjugation by improving solubility and reducing steric constraints. The molecule is widely applicable for coupling warheads to targeting ligands, enabling subsequent click chemistry or further functionalization; detailed structural and reactivity guidance is provided below.
Structure: The linker contains a propargyl (terminal alkyne) moiety connected through a polyethylene glycol chain to a pentafluorophenyl ester. It features an activated carboxylate for acyl transfer and ether linkages within the PEG backbone, yielding a polar, water-compatible scaffold suitable for bioconjugation.
Reactivity: The PFP ester reacts with primary amines to form stable amide bonds via nucleophilic acyl substitution, typically under mild, buffered aqueous or mixed-solvent conditions that maintain amine nucleophilicity while limiting hydrolysis. The terminal alkyne can be carried forward for copper-catalyzed azide–alkyne cycloaddition or related click-compatible steps, using standard catalysts and inert atmosphere practices when required.
* 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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