APN-PEG4-PFP
APN-PEG4-PFP is a polyethylene glycol–based PROTAC linker featuring a four-ethylene glycol chain terminated with a pentafluorophenyl (PFP) ester, which serves as a highly reactive acylating handle for covalent conjugation to primary amines or other nucleophilic residues on targeting ligands and effector modules. Structurally, the PEG segment provides a flexible, hydrophilic spacer that can reduce steric hindrance and help tune the effective distance and orientation between the two binding partners within a ternary-degradation complex. In PROTAC design, this linker enables modular assembly by allowing researchers to attach the PFP-activated end to an amine-bearing ligand, yielding a stable conjugate that can subsequently recruit an E3 ligase or target-binding moiety depending on the chosen partners. Its utility lies in facilitating rapid, reproducible synthesis of linker-defined degraders and in supporting structure–activity optimization by varying PEG length and conjugation chemistry.
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* For research and manufacturing use only. Not for human or clinical use.
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APN-PEG4-PFP is a polyethylene glycol-based PROTAC linker designed to connect ligands while supporting efficient ternary-complex formation through improved solubility and conformational flexibility. Its activated functional group enables robust conjugation to amine- or nucleophile-bearing partners under standard bioconjugation workflows. This product is well suited for researchers constructing targeted protein degraders, where linker integrity and controlled attachment chemistry are critical. Detailed structural and reactivity considerations are provided below.
Structure: The linker comprises a PEG chain providing hydrophilicity and spacing, terminating in a pentafluorophenyl ester motif. The conjugation handle is an activated aromatic ester, enabling nucleophilic acyl substitution. Overall, it behaves as a flexible, water-compatible spacer with an electrophilic carbonyl for linkage formation.
Reactivity: The pentafluorophenyl ester reacts via acyl substitution with primary amines, amino-containing ligands, or other suitable nucleophiles to form stable amide or related acylated linkages. Conjugations are typically performed under mildly basic conditions in polar organic or mixed aqueous buffers, with careful control of pH and stoichiometry to minimize hydrolysis. No special catalysts are generally required; reaction efficiency depends on nucleophile strength and maintaining the activated ester in its reactive state.
* 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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