Methyltetrazine-PEG8-NHS ester
CAS No.: 2183440-34-6
Cat No.: BP-500473
Purity: 98%
4.5 
Methyltetrazine-PEG8-NHS ester is a heterobifunctional PEG-based linker designed for modular PROTAC and targeted degradation construct assembly. Structurally, it combines a methyltetrazine moiety for rapid inverse-electron-demand Diels–Alder reactivity with an NHS ester that readily forms stable amide bonds with primary amines on degrader ligands or other targeting modules. The PEG8 chain provides a flexible, hydrophilic spacer that can reduce steric interference and improve productive orientation between the binding elements, which is critical for efficient ternary complex formation and subsequent ubiquitin–proteasome–mediated degradation. In PROTAC workflows, this reagent enables orthogonal conjugation: the NHS ester allows straightforward attachment to amine-functionalized warheads, while the methyltetrazine handle supports subsequent coupling to trans-cyclooctene–bearing partners under bioorthogonal conditions. Its value lies in simplifying stepwise synthesis, enhancing conjugation efficiency, and supporting systematic linker optimization for mechanistic studies of targeted protein degradation.
Structure of 2183440-34-6
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Methyltetrazine-PEG8-NHS ester is a bifunctional PEG-based linker designed for efficient conjugation in PROTAC workflows, enabling the installation of a methyltetrazine handle alongside an NHS-ester reactive group. Its PEG spacer supports solubility and reduces steric interference during target-binding and ternary-complex formation. The methyltetrazine moiety is suited for bioorthogonal ligation strategies, while the NHS ester facilitates rapid coupling to primary amines. Detailed structural and reactivity considerations are provided below.
Structure: The linker comprises a methyltetrazine functional group connected through a polyethylene glycol spacer to an N-hydroxysuccinimide ester. It contains aromatic heterocycles, an NHS-activated carboxylate, and ether linkages within the PEG chain. These features provide flexible spacing and enhanced aqueous compatibility.
Reactivity: The NHS ester reacts with primary amines via acyl substitution to form stable amide bonds, typically under mildly basic aqueous or mixed solvent conditions. The methyltetrazine group participates in inverse-electron-demand Diels–Alder bioorthogonal ligation with appropriate strained dienes, proceeding without metal catalysts. For PROTAC assembly, sequential coupling is commonly used to first install the amine-bearing partner, then perform the tetrazine ligation under conditions that preserve protein and ligand 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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