Mal-PEG1-PFP ester
CAS No.: 1807530-08-0
Cat No.: BP-500348
Purity: ≥95%
4.5 
Mal-PEG1-PFP ester is a short, heterobifunctional polyethylene glycol linker featuring a maleimide group and a pentafluorophenyl (PFP) ester for orthogonal conjugation. The maleimide moiety enables selective coupling to thiol-containing ligands (for example, cysteine residues or reduced thiol handles) via a Michael-type addition, while the PFP ester is an activated carboxylate that readily reacts with primary amines to form stable amide bonds. In PROTAC and targeted protein degradation workflows, this dual-reactive architecture allows researchers to modularly assemble conjugates by first attaching one component through thiol chemistry and subsequently coupling the second component through amide formation, or vice versa, depending on the desired orientation and linker placement. Its PEG-derived segment provides aqueous solubility and can help reduce steric constraints that may otherwise impair binding to the target protein or the E3 ligase-recruiting moiety, thereby supporting systematic optimization of degrader performance.
Structure of 1807530-08-0
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Mal-PEG1-PFP ester is a multifunctional PEG-based linker designed for constructing PROTACs through efficient, chemoselective conjugation. Its maleimide handle enables rapid coupling to thiol-containing ligands, while the activated PFP ester supports acylation of nucleophilic amines to form stable linkages. This combination facilitates modular assembly of bifunctional degraders with tunable spacing and improved bioconjugation practicality. Detailed structural and reactivity considerations are provided below.
Structure: The linker contains a PEG segment that provides flexible, hydrophilic spacing, coupled to a maleimide electrophile and a pentafluorophenyl-activated ester. It features conjugated aromatic ester functionality and Michael-acceptor double-bond character, enabling selective bond formation with thiols and amines under mild conditions.
Reactivity: The maleimide reacts via thiol–Michael addition, typically promoted in aqueous buffers with controlled pH to preserve thiol nucleophilicity while minimizing side reactions. The PFP ester undergoes nucleophilic acyl substitution with primary amines to generate stable amide bonds; reactions are commonly performed in polar aprotic or mixed aqueous media. Base or catalysts are chosen to balance amine activation and maleimide stability, and freshly prepared thiols are often used for best coupling efficiency.
* 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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