3,4-Dibromo-Mal-PEG2-amine
CAS No.: 1807534-86-6
Cat No.: BP-501204
4.5 
3,4-Dibromo-Mal-PEG2-amine is a bifunctional PEG-based linker bearing a maleimide electrophile and a short ethylene glycol spacer terminated with an amine, with two bromine atoms at the 3,4-positions of the maleimide ring. The 3,4-dibromomaleimide moiety supports characteristic thiol addition/substitution chemistry (for example, cysteine residues on targeting modules or thiol-derivatized binding partners), forming a stable thioether linkage under standard bioconjugation conditions. The PEG2 segment provides aqueous solubility and spatial separation between the conjugated partners, which can reduce steric interference and help maintain productive ternary complex formation in PROTAC workflows. In targeted protein degradation research, this linker is useful for constructing modular PROTACs or related degraders by combining a thiol-reactive dibromomaleimide region with a free terminal amine for a second coupling step, thereby facilitating systematic structure–activity studies and optimization of linker length and electronics for efficient ubiquitin–ligase recruitment and degradation.
Structure of 1807534-86-6
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3,4-Dibromo-Mal-PEG2-amine is a bifunctional, PEG-based PROTAC linker designed to connect a maleimide-bearing core with amine-reactive handles for modular assembly of targeted protein degraders. Its flexible polyethylene glycol spacer supports productive ternary-complex formation by improving solubility and reducing steric constraints around the recruiting warheads. The two brominated positions enable further functional diversification, while the amine functionality facilitates conjugation strategies. The structure and reactivity considerations are described in detail below.
Structure: The linker contains a PEG spacer that imparts conformational flexibility, a 3,4-dibromomaleimide motif capable of thiol addition/substitution, and a terminal amine for further derivatization. The molecule features heteroatoms (oxygen and nitrogen) that enhance polarity and hydrogen-bonding potential, supporting aqueous compatibility.
Reactivity: For PROTAC construction, the maleimide functionality is typically engaged via nucleophilic thiol addition under mild aqueous or mixed-solvent conditions, forming stable thioether linkages. The bromine atoms are located on the maleimide alkene and are not aryl bromides; thiols can react at this dibromomaleimide motif under appropriate conditions. Thiol–dibromomaleimide conjugations are generally performed under mild conditions with controlled pH to favor thiol nucleophilicity; aryl palladium cross-coupling is not the relevant pathway for these bromides.
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Concentration (start) x Volume (start) = Concentration (final) x Volume (final)
It is commonly abbreviated as: C1V1 = C2V2
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