Mal-NH-PEG10-CH2CH2COOPFP ester
Mal-NH-PEG10-CH2CH2COOPFP ester is a heterobifunctional, maleimide-terminated PEG linker designed for PROTAC and targeted protein degradation workflows requiring orthogonal conjugation. The maleimide group provides a highly selective handle for coupling to thiol-containing ligands or cysteine residues on biomolecules, enabling stable thioether formation under mild conditions. The PEG spacer confers aqueous solubility and conformational flexibility, helping to reduce steric interference between the target-binding and E3-recruiting modules and thereby improving productive ternary complex formation. The terminal activated ester (PFP ester) enables efficient acylation of primary amines on amine-bearing partners, allowing sequential or controlled conjugation strategies to assemble multi-component degraders. In research, this linker supports modular synthesis of PROTACs by facilitating reliable attachment of two distinct ligands, while the PEG chain length and dual-reactivity improve reproducibility and experimental throughput in degradation assays.
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* For research and manufacturing use only. Not for human or clinical use.
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This Mal-NH-PEG10-CH2CH2COOPFP ester is a polyethylene glycol (PEG)-based PROTAC linker designed to connect targeting ligands through a maleimide-reactive handle and an activated carboxylate for subsequent conjugation. Its flexible, hydrophilic PEG segment supports productive ternary complex formation by improving solubility and conformational reach, while the electrophilic ester facilitates efficient coupling under standard PROTAC linker assembly workflows. The detailed structural and reactivity considerations are provided below.
Structure: The linker incorporates a PEG chain for hydrophilicity and conformational flexibility, a maleimide-derived electrophile for selective thio-Michael reactivity, and a terminal activated carboxylate ester. It contains amide and ester functionalities, with ether linkages in the PEG backbone that enhance water compatibility and reduce nonspecific aggregation.
Reactivity: PROTAC construction using this linker typically relies on maleimide-thio conjugation (thio-Michael addition) with cysteine-containing ligands or thiolated intermediates, followed by coupling through the activated ester to form stable amide or related linkages with amine-bearing partners. Reactions are commonly performed in aqueous or mixed aqueous buffers at controlled pH, using mild temperatures and inert atmosphere when needed to preserve electrophile integrity. No specific catalyst is generally required, but thiol compatibility and ester stability should be assessed experimentally.
* 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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