N-(Amino-PEG5)-N-bis(PEG4-acid)
CAS No.: 2093152-86-2
Cat No.: BP-501212
4.5 
N-(Amino-PEG5)-N-bis(PEG4-acid) is a heterobifunctional polyethylene glycol (PEG)-based linker featuring one terminal primary amine, two PEG4 carboxylic acid termini, and a central tertiary amine branching point. Structurally, it comprises a PEG5 segment bearing an amino group, flanked by two PEG4 “acid” arms, providing a flexible, hydrophilic, and sterically accommodating scaffold with a defined multivalent geometry. In PROTAC design, this type of linker is used to spatially separate the ligand warhead(s) from the E3 ligase-binding moiety, tuning the effective distance and relative orientation required for productive ternary complex formation. The terminal carboxyl groups enable robust amide-bond formation (or related coupling strategies) to attach to activated functional groups on partner ligands, while the terminal primary amine provides the third direct conjugation site. Its PEG-rich architecture is valuable for improving solubility, reducing nonspecific interactions, and supporting systematic structure–activity relationship studies in targeted protein degradation workflows.
Structure of 2093152-86-2
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This linker, N-(Amino-PEG5)-N-bis(PEG4-acid), is designed to provide a flexible, hydrophilic polyethylene glycol scaffold for building PROTACs. Its polyether architecture supports favorable solubility and linker-mediated spatial control between the target-binding ligand and the E3-recruiting moiety. The amino-functional handle enables robust conjugation strategies, while the PEG-acid termini support established coupling workflows. The following sections describe the structure and practical reactivity considerations in detail.
Structure: The molecule contains an amino-terminated PEG segment connected to a nitrogen center bearing two PEG-acid arms. It is composed primarily of ether linkages within polyethylene glycol chains, with terminal carboxylic acid groups and a primary amine for further functionalization. Overall, it is highly hydrophilic and conformationally flexible.
Reactivity: PROTAC construction using this linker typically relies on amide-bond formation between carboxylic acid termini and complementary amine-bearing ligands, or on coupling of the amino handle to activated carboxyl groups. Suitable approaches include carbodiimide-mediated couplings (often with additives such as HOBt or similar) under aqueous or mixed aqueous/organic conditions, with pH control to balance activation and minimize side reactions. The mechanism proceeds via carboxyl activation followed by nucleophilic acyl substitution to form stable amide linkages.
* 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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