Methylamino-PEG2-acid
CAS No.: 1807503-87-2
Cat No.: BP-501186
4.5 
Methylamino-PEG2-acid is a bifunctional polyethylene glycol (PEG) linker bearing a terminal methylamino group and a carboxylic acid, providing a short, hydrophilic spacer of two ethylene glycol units. The PEG segment imparts aqueous solubility and conformational flexibility, while the acid functionality enables straightforward coupling to PROTAC warheads or ligands through standard amide-forming chemistries, allowing controlled placement of the two binding modules. In PROTAC designs, such linkers help tune the effective distance and relative orientation between the target-binding ligand and the E3 ligase recruiting ligand, thereby improving productive ternary complex formation and degradation efficiency. This linker is particularly useful when minimizing steric interference is critical, because its short PEG chain can balance flexibility with compactness. As a modular building block, it supports systematic structure–activity studies in targeted protein degradation workflows.
Structure of 1807503-87-2
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Methylamino-PEG2-acid is a polyethylene glycol-based PROTAC linker building block designed to provide a hydrophilic, flexible spacer between a ligand and an E3 ligase-recruiting moiety. Its polar ether-rich scaffold and terminal carboxylic acid support robust conjugation strategies that are commonly used to tune solubility, reduce steric congestion, and maintain productive ternary complex formation. Detailed structural and synthetic considerations are provided below.
Structure: The linker comprises a short PEG segment with ether linkages, terminating in a carboxylic acid and bearing a methylamino substituent. This combination yields a polar, hydrogen-bonding-rich scaffold with an amine for derivatization and a carboxyl group for amide formation or activation chemistry, supporting flexible conformational behavior.
Reactivity: The carboxylic acid can be converted to activated intermediates for coupling, enabling formation of amide bonds with amine-bearing ligands under standard peptide-coupling conditions. Typical approaches involve carboxyl activation followed by nucleophilic acyl substitution using an appropriate amine, often in polar aprotic solvents with base to promote reactivity. The methylamino group can be selectively protected or used for orthogonal conjugation depending on the desired PROTAC architecture.
* 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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