3,4-Dibromo-Mal-PEG2-NHBoc
3,4-Dibromo-Mal-PEG2-NHBoc is a dibrominated maleimide–PEG linker bearing a Boc-protected amine, designed to enable robust, modular assembly of PROTACs and related targeted protein degradation constructs. The maleimide core provides a highly selective electrophile for conjugation to thiol-containing ligands (for example, cysteine- or thiol-functionalized binding motifs), while the PEG2 segment offers aqueous solubility and spatial separation to help preserve productive ternary-complex formation. The two bromine substituents on the maleimide framework serve as handles for further synthetic diversification, allowing researchers to tune linker reactivity or incorporate additional functional groups during PROTAC synthesis. In targeted degradation workflows, this linker facilitates controlled attachment of a targeting moiety to a second component, improving the ability to position the recruited E3 ligase-binding element for efficient ubiquitination. As a versatile intermediate, it supports rapid structure–activity exploration and optimization of linker length and conjugation chemistry in degradation research.
Structure of 1807537-43-4
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* For research and manufacturing use only. Not for human or clinical use.
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This PROTAC linker, 3,4-Dibromo-Mal-PEG2-NHBoc, is designed to provide a PEG-based spacer coupled to a protected amine handle and a reactive dibrominated maleimide motif. Its combination supports efficient attachment to targeting ligands and controlled assembly of bifunctional degraders, helping tune physicochemical properties such as solubility and linker flexibility. The following sections describe the structure and practical reactivity considerations for PROTAC construction in detail below.
Structure: The linker contains a PEG spacer that imparts aqueous compatibility and conformational flexibility, connected to a maleimide-derived core bearing two bromine substituents. A Boc-protected amine provides a stable, masked nucleophile, while the maleimide framework offers electrophilic character for subsequent bioconjugation chemistry.
Reactivity: For PROTAC synthesis, the Boc group is typically removed under standard acidolysis conditions to reveal an amine for coupling steps. The dibrominated maleimide portion can participate in electrophile-driven conjugation strategies commonly used to connect ligands through nucleophilic substitution or related maleimide-reactive pathways. Selection of solvent and base is guided by compatibility with the protecting group and the coupling chemistry used for the target-binding moieties.
* 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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