Pyrene azide 3 is an aryl azide linker building block incorporating a pyrene fluorophore and an azide functional group, enabling robust photoinduced or click-compatible conjugation chemistry. Structurally, it provides a rigid aromatic handle for strong fluorescence and a reactive azide “warhead” that can be used to connect PROTAC components through azide-reactive partners (e.g., via copper-catalyzed azide–alkyne cycloaddition or related bioorthogonal strategies, depending on the complementary group). In PROTAC design, such linkers are valuable for positioning the degrader moieties while preserving the binding geometry required for ternary complex formation; the pyrene unit additionally supports sensitive tracking of conjugation efficiency and linker stability by fluorescence readout. This product is therefore useful for researchers developing targeted protein degradation constructs, particularly when monitoring synthesis, optimizing linker length/rigidity, or validating cellular uptake and localization of PROTAC intermediates and final conjugates.
Structure of 2252168-06-0
* For research and manufacturing use only. Not for human or clinical use.
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This pyrene azide linker is designed for efficient incorporation into PROTAC constructs, enabling bioorthogonal installation of linker segments that support targeted protein degradation workflows. Its aromatic pyrene scaffold provides strong hydrophobic character and useful spectroscopic handles, while the azide functionality enables selective conjugation under mild conditions. The points below describe the molecule’s structure and the practical reactivity considerations for PROTAC assembly in research settings.
Structure: The linker contains a polycyclic aromatic pyrene core connected to an azide group. It features conjugated aromatic π-systems and an N3 functional group suitable for click-type transformations. Overall, it is a rigid, hydrophobic aromatic scaffold with a terminal azide for chemoselective reactivity.
Reactivity: The azide group is suitable for copper-catalyzed azide–alkyne cycloaddition or strain-promoted azide–alkyne cycloaddition, depending on the PROTAC design. Typical approaches use an appropriate alkyne partner (often a terminal alkyne or cyclooctyne derivative), with Cu(I) generation from copper salts under standard click conditions for the CuAAC route. For SPAAC, catalyst-free conditions can be used to reduce metal exposure, using polar organic solvents or buffered aqueous mixtures compatible with sensitive ligands.
* 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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