Methyltetrazine-PEG4-acid
CAS No.: 1802907-91-0
Cat No.: BP-500606
Purity: 95%
4.5 
Methyltetrazine-PEG4-acid is a bifunctional PROTAC linker featuring a methyltetrazine reactive handle conjugated to a short polyethylene glycol spacer terminating in a carboxylic acid. The PEG4 chain provides hydrophilicity and conformational flexibility, which can improve solubility and reduce steric interference between the two PROTAC partners during synthesis and biological evaluation. The methyltetrazine moiety is designed for inverse-electron-demand Diels–Alder ligation with strained dienes such as trans-cyclooctene, enabling rapid, bioorthogonal conjugation to generate well-defined heterobifunctional degraders. The terminal acid allows further coupling to amine- or hydrazide-bearing ligands, facilitating modular assembly of target-binding and E3-recruiting components. This linker is valuable for targeted protein degradation research because it supports efficient, chemoselective synthesis of PROTACs under mild conditions, helping researchers tune linker length and attachment chemistry to optimize degradation potency and selectivity.
Structure of 1802907-91-0
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Methyltetrazine-PEG4-acid, is designed to connect a tetrazine-based handle to a PEG-derived spacer terminating in a carboxylic acid functionality. Its key features include a bioorthogonal tetrazine motif for rapid conjugation and a flexible polyethylene glycol segment that can improve solubility and reduce steric constraints during ternary complex formation. The acid terminus enables straightforward coupling to targeting ligands, facilitating modular PROTAC assembly. Detailed structural and reactivity guidance is provided below.
Structure: The linker comprises a methyltetrazine core linked through a PEG chain to a terminal carboxylic acid. It contains heteroaromatic nitrogen-rich rings, ether linkages within the PEG, and a carboxylic acid for derivatization. Overall polarity and conformational flexibility are characteristic of PEG spacers.
Reactivity: Tetrazine functionality supports bioorthogonal inverse-electron-demand Diels–Alder ligation with strained dienes (commonly trans-cyclooctene derivatives), enabling fast, catalyst-free conjugation under mild aqueous conditions. The carboxylic acid can be activated for amide or ester formation using standard coupling chemistries, typically employing carbodiimide reagents with an appropriate base in compatible solvents. Reaction design should prioritize maintaining tetrazine integrity and minimizing conditions that promote hydrolysis or decomposition.
* 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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