Propargyl-PEG2-amine is a short, flexible polyethylene glycol (PEG) linker bearing a terminal propargyl (alkyne) group and a primary amine. Structurally, it provides a hydrophilic, conformationally mobile spacer that can be used to connect PROTAC components while minimizing steric interference at the binding interfaces. The propargyl functionality enables chemoselective conjugation via copper-catalyzed azide–alkyne cycloaddition or related alkyne click strategies, allowing attachment to azide-functional ligands or handles commonly used in targeted degradation constructs. The terminal amine allows further derivatization (e.g., amide coupling to activated carboxylic acids or attachment to activated esters), supporting modular synthesis of bifunctional degraders. In PROTAC research, this linker is valuable for tuning effective distance and orientation between the E3 ligase-recruiting moiety and the target-binding ligand, thereby improving degraders’ synthesis feasibility and facilitating systematic structure–activity studies.
Structure of 944561-44-8
* For research and manufacturing use only. Not for human or clinical use.
| Size | Price | Stock | Quantity |
|---|---|---|---|
| -- | $-- | In stock |
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| ConcentrationVolumeMass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 6.9842 mL | 34.9211 mL | 69.8422 mL |
| 5 mM | 1.3968 mL | 6.9842 mL | 13.9684 mL |
| 10 mM | 0.6984 mL | 3.4921 mL | 6.9842 mL |
Propargyl-PEG2-amine is a PEG-based bifunctional linker designed for modular assembly of PROTACs, enabling efficient spatial separation between a target-binding ligand and an E3 ligase recruiter. Its ether-rich chain provides conformational flexibility and improved solubility, while the terminal alkyne handle supports orthogonal conjugation strategies. These features make it a practical building block for constructing targeted protein degraders, with detailed structural and synthetic considerations provided below.
Structure: The molecule contains a short poly(ethylene glycol) ether segment linked to a primary amine and a propargyl (terminal alkyne) functionality. It features C–N and C–C bonds, ether linkages, and an alkyne capable of selective coupling. The PEG segment imparts hydrophilicity and flexible, solvated conformations.
Reactivity: The terminal alkyne enables click-type conjugations and related alkyne-reactive chemistries, typically proceeding via copper-catalyzed azide–alkyne cycloaddition or catalyst-free variants depending on the partner. The primary amine can be used for amide formation, carbamate/urea coupling, or reductive amination to connect PROTAC fragments. Common approaches use standard coupling reagents in polar organic or mixed solvent systems under conditions 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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