TCO-PEG2-amine
CAS No.: 2141981-87-3
Cat No.: BP-501463
Purity: 95%
4.5 
TCO-PEG2-amine is a bifunctional, polyethylene glycol–containing linker bearing a trans-cyclooctene (TCO) moiety and a terminal primary amine. Structurally, it provides a short PEG spacer that improves aqueous solubility and reduces steric constraints, while the TCO handle enables rapid, catalyst-free bioorthogonal ligation via inverse-electron-demand Diels–Alder chemistry with tetrazine-functional partners. The terminal amine offers a practical conjugation site for coupling to activated carboxyl groups or other electrophiles, allowing researchers to attach the linker to targeting ligands (e.g., small molecules or peptides) or to connect it to PROTAC scaffold components. In targeted protein degradation workflows, this linker is valuable for modular assembly of TCO–tetrazine conjugates, enabling controlled formation of heterobifunctional constructs and facilitating optimization of linker length and flexibility to tune ternary complex formation. Its PEG-mediated spacing and orthogonal reactivity support reproducible, efficient conjugation for mechanistic and optimization studies.
Structure of 2141981-87-3
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* For research and manufacturing use only. Not for human or clinical use.
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TCO-PEG2-amine is a bifunctional PROTAC linker designed to connect targeting ligands through a polyethylene glycol spacer while providing a reactive trans-cyclooctene (TCO) handle for efficient bioorthogonal conjugation. Its flexible PEG architecture supports favorable linker dynamics, and the TCO moiety enables rapid, catalyst-free coupling in PROTAC assembly workflows. The points below describe its structure and practical reactivity considerations in detail.
Structure: The linker contains a trans-cyclooctene functional group coupled to a short polyethylene glycol chain terminating in a primary amine. It features an olefinic cyclooctene motif, ether linkages within the PEG segment, and a terminal amine capable of forming amide or urea derivatives.
Reactivity: TCO-PEG2-amine is commonly used in PROTAC construction via bioorthogonal trans-cyclooctene chemistry, typically reacting with tetrazine-functional partners through a fast inverse-electron-demand Diels–Alder mechanism. Conjugation is generally performed under mild, aqueous-compatible conditions without added catalysts, with solvent choice guided by solubility of both partners. The terminal amine can also be used for standard amide-forming coupling strategies when paired with activated carboxylic acid derivatives.
* 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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