Hydroxy-PEG4-methylamine
CAS No.: 90430-59-4
Cat No.: BP-501051
4.5 
Hydroxy-PEG4-methylamine is a hydroxy-terminated polyethylene glycol linker bearing a terminal methylamine functionality, corresponding to a short, flexible PEG chain that can be used to connect PROTAC-relevant building blocks through stable covalent chemistry. Structurally, it provides a hydrated, conformationally mobile spacer that can reduce steric clashes between the ligand-binding domains of a PROTAC and help preserve productive geometry for ternary complex formation. The terminal hydroxyl group enables derivatization (for example, via activation/ether or ester formation depending on the synthetic strategy), while the methylamine can serve as a nucleophilic handle for amide coupling or other amine-reactive conjugation routes. In targeted protein degradation research, such PEG-based linkers are widely employed to tune linker length, polarity, and flexibility, thereby improving solubility and often enhancing degradation performance by facilitating effective recruitment of the target protein while maintaining favorable interactions with the E3 ligase ligand.
Structure of 90430-59-4
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Hydroxy-PEG4-methylamine is a polyethylene glycol-based linker building block designed to support PROTAC assembly by providing a hydrophilic, flexible spacer between targeting and recruiting ligands. Its ether-rich PEG framework can enhance solubility and help tune linker length and conformational freedom, which are key factors for effective ternary complex formation. The following sections describe the linker’s structure and the practical considerations for its incorporation into PROTAC constructs.
Structure: The molecule features a hydroxy-terminated PEG chain with repeating ether units and a terminal methylamine functionality. Its backbone is dominated by C–O ether linkages, with an alcohol and a primary amine enabling hydrogen bonding and polarity-driven solvation, consistent with PEG-like physical behavior.
Reactivity: The terminal methylamine can participate in nucleophilic substitution or amide/urea-forming coupling after appropriate activation of a carboxylic acid or activated ester on a partner ligand. The hydroxy group can be used for further derivatization via standard ether or carbonate-forming strategies. Typical PROTAC linker conjugations are performed under mild base and coupling conditions in common organic solvents, with reaction progress monitored by chromatography or mass spectrometry.
* 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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