Methylamino-PEG2-t-butyl ester
CAS No.: 1807521-04-5
Cat No.: BP-500495
Purity: ≥95%
4.5 
Methylamino-PEG2-t-butyl ester is a short, hydrophilic polyethylene glycol–based linker featuring a terminal methylamino group and a t-butyl ester that serves as a protected carboxyl functionality. The PEG2 segment provides a flexible, water-soluble spacer that can reduce steric interference between the two ligands typically used in PROTACs, while the methylamino handle enables straightforward conjugation strategies such as amide or carbamate formation after appropriate activation. The t-butyl ester is commonly employed to mask an acidic group during synthesis and can be selectively deprotected under conditions compatible with downstream coupling, allowing installation of the linker attachment point to either the targeting ligand or the E3-recruiting moiety. In targeted protein degradation research, this linker supports efficient molecular proximity and productive ternary complex formation by tuning distance and conformational freedom between partners, improving the likelihood of ubiquitination and subsequent proteasomal degradation. Its compact PEG architecture makes it particularly useful when minimizing overall size while maintaining aqueous handling and synthetic modularity.
Structure of 1807521-04-5
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Methylamino-PEG2-t-butyl ester is a PEG-based PROTAC linker designed to provide a hydrophilic, conformationally flexible connection between a ligand and an E3-recruiting or target-binding module. Its ester functionality supports controlled derivatization and subsequent coupling strategies commonly used in targeted protein degradation workflows. The following points describe its structure-related features and practical reactivity considerations for PROTAC assembly in the laboratory.
Structure: The linker comprises a short polyethylene glycol segment bearing a methylamino substituent and a tert-butyl ester group. It contains ether linkages within the PEG chain, an amide-forming methylamino functionality, and an ester carbonyl. Overall, it offers polarity and flexibility while maintaining a protected carboxylate handle.
Reactivity: The tert-butyl ester is well suited to acid-labile deprotection, enabling generation of a reactive carboxylic acid for subsequent coupling to amines or other nucleophiles used in PROTAC synthesis. Typical approaches employ mild acid conditions for ester cleavage, followed by standard amide-formation chemistries (e.g., carbodiimide-mediated coupling) in compatible organic solvents. The methylamino group can participate as a nucleophile under appropriate activation, supporting selective conjugation strategies.
* 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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