Mal-PEG2-oxyamine
Mal-PEG2-oxyamine is a heterobifunctional polyethylene glycol linker featuring a maleimide electrophile at one terminus and a terminal oxyamine nucleophile at the other, enabling orthogonal conjugation chemistry in PROTAC and targeted degradation workflows. The maleimide group selectively reacts with thiols on cysteine residues or thiol-containing handles, allowing efficient attachment to protein binders, engineered degron scaffolds, or cysteine-functionalized targeting ligands under mild aqueous conditions. The oxyamine terminus provides a complementary reactive handle for subsequent coupling to carbonyl-bearing partners or for installing the linker into larger degraders through established oxime/oxime-like conjugation strategies. With a short PEG chain, it offers modest hydrophilicity and spatial separation to reduce steric interference while maintaining synthetic tractability. This linker is valuable for constructing multi-component targeted degraders, facilitating controlled assembly of conjugates and enabling systematic structure–activity studies on linker length and attachment geometry.
Structure of 1146245-73-9
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Mal-PEG2-oxyamine is a bifunctional PEG-based linker designed for efficient conjugation in targeted protein degradation workflows. Its maleimide handle enables selective coupling to thiol-bearing ligands, while the terminal oxyamine supports subsequent amide/oxime-compatible assembly strategies commonly used to build PROTAC architectures. The resulting linkers can help tune physicochemical properties such as solubility and linker flexibility, supporting robust synthesis and reliable performance in degradation studies. Detailed structural and reactivity considerations are provided below.
Structure: The linker contains a maleimide moiety for thiol-reactive chemistry and a short polyethylene glycol segment that imparts hydrophilicity and conformational flexibility. An oxyamine functional group provides additional orthogonal reactivity for downstream coupling steps. Its conjugation-ready design relies on stable heteroatom-rich linkages.
Reactivity: Maleimide groups typically react with free thiols under mild aqueous or mixed solvent conditions, often near neutral pH, via a Michael-type addition that yields a stable thioether adduct. For PROTAC synthesis, the thiol-bearing partner is commonly introduced first, followed by reaction of the oxyamine functionality with an appropriately activated electrophile (e.g., amide-forming reagents or compatible carbonyl/derivatization partners). Mild bases and buffered media are frequently used to preserve functional-group integrity.
* 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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