Mal-NH-PEG16-CH2CH2COOPFP ester
Mal-NH-PEG16-CH2CH2COOPFP ester is a heterobifunctional, maleimide-terminated polyethylene glycol (PEG) linker designed for PROTAC and targeted protein degradation workflows. Structurally, it combines a maleimide reactive handle with a PEG chain of extended length and a terminal carboxylate activated as an ester, providing both aqueous solubility and orthogonal conjugation sites. In PROTAC assembly, the maleimide group enables selective Michael-type addition to thiol-containing ligands (e.g., cysteine- or engineered thiol-bearing warheads or E3 ligands), forming a stable thioether linkage that connects the targeting module to the linker. The PEG spacer helps tune effective molarity and reduces steric constraints, while the terminal activated ester can be used to couple to amine-bearing partners or to further derivatize the construct for subsequent conjugation steps. This linker is valuable for generating well-defined, modular degradation agents with improved handling properties and controlled geometry for studying ternary complex formation.
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* For research and manufacturing use only. Not for human or clinical use.
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This PEG-based PROTAC linker, Mal-NH-PEG16-CH2CH2COOPFP ester, is designed to connect a maleimide-bearing handle to a reactive carboxylate functionality, enabling efficient assembly of targeted protein degradation constructs. Its hydrophilic PEG segment supports favorable solubility and linker flexibility, while the electrophilic ester moiety provides a practical point for coupling to amine- or nucleophile-containing ligands. The following sections describe the linker’s structure and the reactivity principles relevant to PROTAC synthesis.
Structure: The linker contains a maleimide-derived electrophilic core, a poly(ethylene glycol) spacer, and a terminal propyl/alkyl carboxylate ester motif. It features multiple ether linkages within the PEG chain, along with amide and ester functionalities that contribute to polarity, conformational flexibility, and stable covalent connectivity during PROTAC construction.
Reactivity: The maleimide portion is typically used for selective thiol–maleimide conjugation via Michael addition under mildly basic aqueous conditions, forming a stable thioether linkage. The terminal ester (PFP-ester type) is suited for acyl transfer or nucleophilic substitution with appropriate amines or other nucleophiles to install ligand fragments. Common approaches use buffered aqueous/organic solvent mixtures, with careful control of pH to balance maleimide reactivity and 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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