Pyrene-amido-PEG4-azide
Pyrene-amido-PEG4-azide is a heterobifunctional PEG-based linker that combines a terminal azide handle with a fluorescent pyrene reporter and an amide linkage to the PEG chain, providing a practical tool for PROTAC and targeted protein degradation workflows. The PEG4 segment offers aqueous solubility and conformational flexibility, helping to reduce steric interference between the two PROTAC arms. The azide group enables reliable bioorthogonal conjugation (commonly via copper-free azide–alkyne cycloaddition or related click chemistries) to install the linker onto a warhead or recruiting ligand bearing a complementary alkyne functionality. In parallel, the pyrene moiety serves as a spectroscopic tag to monitor conjugation efficiency and, when incorporated into degradation constructs, to support tracking of assembly and cellular uptake. This linker is therefore valuable for researchers optimizing PROTAC architecture, verifying synthetic yields, and improving experimental readouts during targeted degradation studies.
Structure of 1817735-36-6
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* For research and manufacturing use only. Not for human or clinical use.
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Pyrene-amido-PEG4-azide is a bifunctional PEG-based PROTAC linker designed to combine a photoactive/fluorescent pyrene handle with an azide for modular conjugation. Its amide-linked PEG segment provides conformational flexibility and improved solubility, supporting efficient formation of ternary complexes in targeted protein degradation workflows. The pyrene moiety additionally enables monitoring of conjugation and linker behavior, while the azide enables robust click-based assembly. Detailed structural and reactivity considerations are provided below.
Structure: The linker comprises a pyrene aromatic group connected through an amide to a polyethylene glycol chain terminated by an azide. It contains an aromatic system, amide linkage, ether-rich PEG segments, and an azide functional group. These features confer hydrophilicity, flexibility, and stable covalent connectivity for PROTAC assembly.
Reactivity: The azide participates in copper-catalyzed azide–alkyne cycloaddition or related strain-promoted azide chemistry to form stable triazole linkages. PROTAC construction typically involves preparing an alkyne-bearing warhead or ligand, then coupling under conditions compatible with amide and PEG stability. Common approaches use Cu(I) generated in situ with appropriate ligands, or copper-free click variants in polar solvents to minimize side reactions and preserve sensitive functional groups.
* 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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