Tetrazine-Amine
CAS No.: 1092689-33-2
Cat No.: BP-502178
4.5 
Tetrazine-Amine is a bifunctional PROTAC linker building block combining an electron-deficient tetrazine moiety with a terminal amine handle. Structurally, it provides a short, chemically defined conjugation “bridge” that can be incorporated into targeted protein degradation constructs by coupling the amine to a complementary reactive group on either the ligand-bearing warhead or the E3-ligase–recruiting component. The tetrazine functionality enables rapid, bioorthogonal inverse-electron-demand Diels–Alder reactivity with trans-cyclooctene or related strained alkenes, allowing researchers to assemble or exchange PROTAC components under mild conditions while minimizing nonspecific reactions. In PROTAC design, this linker supports modular synthesis, flexible optimization of linker length and attachment geometry, and controlled formation of the final conjugate that promotes productive ternary-complex formation. As a result, Tetrazine-Amine is valuable for developing and troubleshooting targeted degradation workflows that require efficient conjugation and reliable construct assembly for mechanistic and optimization studies.
Structure of 1092689-33-2
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Tetrazine-Amine is a bifunctional linker designed to enable modular assembly of PROTACs by connecting a tetrazine-reactive handle with an amine for further conjugation to targeting ligands. Its use supports efficient, chemoselective coupling strategies that can improve synthetic flexibility and streamline the preparation of targeted protein degraders. The following points describe the molecule’s structure-related features and practical reactivity considerations for PROTAC construction in detail below.
Structure: The linker contains a tetrazine motif paired with a primary amine functionality, providing orthogonal reactivity for stepwise synthesis. It is characterized by heteroaromatic nitrogen-rich ring chemistry and an amine capable of forming stable covalent linkages under standard coupling conditions. Overall, it is suited for aqueous-compatible conjugation workflows.
Reactivity: Tetrazine groups typically undergo rapid inverse-electron-demand cycloaddition with strained dienes such as trans-cyclooctene or related cyclooctene derivatives, enabling bioorthogonal ligation. The amine handle can be used for nucleophilic substitution or amide/urea-forming coupling to attach targeting ligands or other PROTAC components. Common approaches employ mild bases and coupling reagents in polar aprotic or buffered aqueous media, with purification by standard chromatographic methods to remove unreacted partners.
* 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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