Mal-PFP ester
CAS No.: 138194-55-5
Cat No.: BP-501540
4.5 
Mal-PFP ester is a maleimide-activated linker designed for efficient conjugation in targeted protein degradation workflows. Structurally, it contains a maleimide electrophile that undergoes rapid, chemoselective addition with thiol-containing partners (for example, cysteine residues or engineered thiol tags), enabling stable thioether bond formation. The “PFP ester” functionality provides an additional acylating handle that can react with nucleophiles such as primary amines, allowing modular assembly of bifunctional constructs. In PROTAC design, Mal-PFP ester serves as a versatile bridging element that connects a protein-binding ligand to a degrader module while preserving the geometry and flexibility needed for productive ternary complex formation. Its dual-reactivity supports streamlined synthesis of linker-ligand conjugates, which is valuable for rapid prototyping, systematic structure–activity studies, and optimization of linker length and attachment chemistry in targeted degradation research.
Structure of 138194-55-5
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Mal-PFP ester is a versatile electrophilic linker building block designed for efficient conjugation in PROTAC assembly. Its activated ester functionality enables robust coupling to nucleophilic groups on partner ligands, supporting the modular synthesis of targeted protein degraders. The linker’s reactivity and compatibility with common organic synthesis workflows provide practical advantages for constructing PROTACs under controlled conditions. Detailed structural and reactivity considerations are provided below.
Structure: Mal-PFP ester contains a maleimide-derived scaffold bearing an activated pentafluorophenyl ester. The molecule features an electrophilic ester carbonyl, aromatic pentafluorophenyl leaving group, and a conjugated maleimide motif. This combination yields a stable, isolable electrophile suited for selective acyl transfer chemistry.
Reactivity: The PFP ester can undergo acyl substitution with nucleophiles such as amines, alcohols, or thiols to form stable amide or related linkages commonly used in PROTAC construction. Typical conditions employ dry organic solvents with mild base to generate the nucleophile, while protecting groups may be used to preserve sensitive functionalities. Reaction progress is monitored by standard analytical methods, and purification is performed to remove unreacted ester and 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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