Mal-PEG5-acid is a heterobifunctional polyethylene glycol (PEG) linker featuring a terminal maleimide group for chemoselective conjugation to thiols and a terminal carboxylic acid for subsequent coupling or attachment to PROTAC scaffolds. The PEG chain length provides a flexible, hydrophilic spacer that can reduce steric interference and improve the effective reach between the ligand-binding moiety and the recruited E3 ligase component. In PROTAC design, the maleimide enables stable thioether formation with cysteine-containing ligands or thiol-functionalized intermediates, while the carboxyl group offers a handle for amide coupling to incorporate the linker into larger constructs. This linker is particularly valuable for constructing modular targeted protein degradation molecules where controlled geometry and aqueous solubility are critical for maintaining binding, promoting ternary complex formation, and supporting efficient degradation in cell-based assays.
Structure of 1286755-26-7
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| Size | Price | Stock | Quantity |
|---|---|---|---|
| -- | $-- | In stock |
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| ConcentrationVolumeMass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.5681 mL | 12.8403 mL | 25.6805 mL |
| 5 mM | 0.5136 mL | 2.5681 mL | 5.1361 mL |
| 10 mM | 0.2568 mL | 1.2840 mL | 2.5681 mL |
This Mal-PEG5-acid linker is designed for efficient conjugation in targeted protein degradation workflows, enabling robust attachment of ligands to generate PROTAC constructs. Its PEG-based spacer provides favorable solubility and conformational flexibility, while the maleimide functionality supports selective coupling to thiol-bearing partners under mild conditions. The resulting linkages can improve the practical assembly of degraders and support systematic structure–activity exploration; the following sections describe its structure and reactivity in detail below.
Structure: Mal-PEG5-acid comprises a maleimide electrophile linked to a poly(ethylene glycol) spacer terminating in a carboxylic acid. The maleimide ring contains activated double bonds for thiol addition, while the PEG chain provides ether-rich, flexible connectivity. The carboxyl group offers an anionic handle for downstream coupling and salt formation.
Reactivity: The maleimide group reacts with sulfhydryl-containing nucleophiles via a Michael-type addition to form a stable thioether linkage. Suitable conditions typically use aqueous or mixed aqueous buffers at near-neutral pH, with controlled temperature and exclusion of competing thiols. Common solvents include water, buffered aqueous media, and compatible co-solvents used for solubilizing ligands. No specialized catalysts are generally required; reaction rate and selectivity depend on thiol availability and buffer composition.
* 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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