Diketone-PEG4-PFP ester
CAS No.: 2353409-84-2
Cat No.: BP-501307
4.5 
Diketone-PEG4-PFP ester is a heterobifunctional PROTAC linker featuring a PEG4 spacer that connects a β-diketone metal-chelating motif to a pentafluorophenyl (PFP) ester electrophile. The diketone functionality can coordinate metal ions and is widely used in targeted conjugation strategies where controlled association or stabilization of a ligand–metal–protein interface is beneficial. The PFP ester provides an activated carboxylate for efficient nucleophilic acyl substitution with primary amines (for example, lysine residues or amine-bearing targeting ligands), enabling robust formation of amide bonds under standard bioconjugation conditions. In PROTAC design, this linker can be used to spatially tune the distance and flexibility between a protein-binding ligand and a second functional element, while the PEG segment improves solubility and reduces nonspecific aggregation. The result is a versatile tool for constructing and optimizing targeted protein degradation probes and for systematically evaluating how linker geometry influences ternary complex formation and degradation efficiency.
Structure of 2353409-84-2
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Diketone-PEG4-PFP ester is a PEG-based linker designed for constructing PROTACs through efficient amide-forming coupling with primary amine–bearing ligands. Its PEG spacer supports favorable solubility and conformational flexibility, while the PFP ester provides a highly reactive electrophile for rapid conjugation under mild conditions. This product is particularly useful when assembling targeted protein degraders where controlled linker attachment and reliable chemistry are critical; detailed structural and reactivity considerations are provided below.
Structure: The linker comprises a PEG spacer terminated by a pentafluorophenyl (PFP) ester and includes a diketone motif. It contains ether linkages within the polymer chain and an activated ester functional group, enabling stable conjugate formation. Overall polarity and hydrogen-bonding capacity support aqueous compatibility.
Reactivity: The PFP ester typically reacts with primary amines to form amide bonds via nucleophilic acyl substitution. Suitable conditions commonly involve an amine nucleophile, a compatible base, and aqueous or mixed aqueous/organic solvents at mild temperature to preserve sensitive ligands. No special catalysts are required; reaction rate is driven by the PFP leaving group. After coupling, purification is usually performed to remove hydrolyzed ester byproducts.
* 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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