N-(m-PEG4)-3,3-Dimethyl-3H-indole-N'-(acid-PEG3)-benzothiazole
N-(m-PEG4)-3,3-Dimethyl-3H-indole-N'-(acid-PEG3)-benzothiazole is a heterobifunctional PROTAC linker built from two PEG segments that provide solubility and conformational flexibility while separating functional pharmacophores. Structurally, it contains a cyanine-like conjugated indolium/benzothiazolium dye core bearing an acid-terminated PEG3 substituent on the benzothiazolium nitrogen and an m-PEG4 substituent on the indolium nitrogen, rather than an amide-linked indole–benzothiazole core. In PROTAC design, such linkers act as molecular “spacers” that position the E3-ligase-binding moiety and the target-binding ligand for productive engagement, thereby improving the probability of stable ubiquitin-recruiting complex assembly. The PEG architecture is particularly valuable for aqueous handling and for optimizing degradation efficiency across different target-ligand geometries. This linker is therefore a useful building block for constructing and systematically comparing targeted protein degradation constructs in vitro.
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* For research and manufacturing use only. Not for human or clinical use.
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This PEG-based PROTAC linker, N-(m-PEG4)-3,3-Dimethyl-3H-indole-N'-(acid-PEG3)-benzothiazole, is designed to provide a flexible, water-compatible connection between targeting and E3-ligase-binding modules. Its ether-rich polyethylene glycol segments support solubility and conformational adaptability, which can improve productive ternary complex formation in targeted protein degradation workflows. The following points describe its structure and practical reactivity considerations for PROTAC assembly in research settings.
Structure: The linker contains two polyethylene glycol segments connected through aromatic scaffolds, incorporating an indole and a benzothiazole motif. Ether linkages confer flexibility and hydrophilicity, while the presence of an acid-terminated PEG handle enables stable amide formation. Overall, it is a polar, conformationally adaptable bioconjugation platform.
Reactivity: The acid-PEG3 terminus is suitable for coupling reactions that form amide bonds with complementary amine-bearing ligands, using standard peptide-coupling chemistries. Typical conditions rely on activating the carboxylic acid (for example, carbodiimide or uronium-type activation) in polar aprotic or mixed aqueous solvents, often with a base to promote nucleophilic acyl substitution. The flexible PEG spacers generally tolerate mild coupling conditions without disrupting aromatic heterocycles.
* 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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