Hydroxy-PEG3-C2-PFP ester
CAS No.: 1807537-40-1
Cat No.: BP-501614
Purity: ≥95%
4.5 
Hydroxy-PEG3-C2-PFP ester is a bifunctional polyethylene glycol (PEG) linker featuring a terminal hydroxyl group and an activated pentafluorophenyl (PFP) ester for acyl transfer. Structurally, it provides a short, flexible PEG3 spacer connected through a C2 linker segment, enabling controlled separation between a PROTAC warhead (or other targeting moiety) and the conjugation site on the partner ligand. In PROTAC design, the PFP ester serves as a highly reactive electrophile that can be selectively acylated by nucleophilic groups such as primary amines or appropriate hydroxyl/thiol functionalities, forming a stable amide or related linkage while the PEG segment improves solubility and reduces steric constraints. This linker is valuable for constructing targeted protein degradation probes where tuning the linker length and flexibility is critical for maintaining binding to both the target protein and the E3 ligase, thereby supporting systematic optimization of degradation potency and selectivity.
Structure of 1807537-40-1
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Hydroxy-PEG3-C2-PFP ester is a PEG-based PROTAC linker designed to connect targeting ligands under conditions compatible with common bioconjugation workflows. Its polyethylene glycol segment provides beneficial solubility and conformational flexibility, while the activated PFP ester enables efficient coupling to nucleophilic groups on proteins, peptides, or small-molecule handles. The molecule is therefore well suited for assembling PROTAC architectures where reliable linker installation and downstream conjugation are required; the following points describe its structure and practical reactivity in detail below.
Structure: The linker comprises a hydroxy-terminated polyethylene glycol chain coupled through a short spacer to a pentafluorophenyl (PFP) ester. It contains ether linkages typical of PEG, an ester carbonyl, and aromatic pentafluorophenyl substituents that activate the acyl group toward nucleophilic substitution. Overall, it is a polar, flexible scaffold.
Reactivity: The PFP ester is an activated carboxylate designed for acyl substitution by nucleophiles such as primary amines and, under appropriate conditions, other suitable nucleophiles. PROTAC synthesis typically employs mild base and anhydrous or low-water organic solvent systems to balance reactivity and stability, with the reaction proceeding via formation of a tetrahedral intermediate followed by departure of the pentafluorophenolate leaving group. Reaction monitoring by standard analytical methods is recommended to optimize 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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