Bis-Mal-Lysine-PEG4-acid

 CAS No.: 1426164-52-4  Cat No.: BP-500948 4.5  

Bis-Mal-Lysine-PEG4-acid is a bifunctional, PEG-based PROTAC linker built around a lysine core bearing two maleimide-reactive termini and a terminal carboxylic acid for downstream conjugation or handle-based purification. The PEG4 spacer provides aqueous solubility and conformational flexibility, helping to tune the effective distance and orientation between a warhead-bearing component and a second binding module in targeted protein degradation constructs. In PROTAC workflows, the maleimide groups enable chemoselective conjugation to thiols (for example, cysteine-containing ligands or engineered thiol tags) under mild conditions, allowing modular assembly of heterobifunctional degraders. The lysine-derived bis-functional architecture supports higher local effective molarity and can facilitate controlled stoichiometry when linking two biomolecular fragments. This linker is valuable for researchers optimizing linker length, hydrophilicity, and conjugation efficiency to improve degradation potency and selectivity in targeted protein degradation studies.

Bis-Mal-Lysine-PEG4-acid

Structure of 1426164-52-4

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PROTAC Linker
Molecular Formula
C₃₁H₄₅N₅O₁₃
Molecular Weight
695.71

* For research and manufacturing use only. Not for human or clinical use.

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IUPACName
3-[2-[2-[2-[2-[2,6-bis[3-(2,5-dioxopyrrol-1-yl)propanoylamino]hexanoylamino]ethoxy]ethoxy]ethoxy]ethoxy]propanoic acid
InChI Key
RZAXBVRZUKAYCY-UHFFFAOYSA-N
InChI
InChI=1S/C31H45N5O13/c37-24(8-13-35-26(39)4-5-27(35)40)32-11-2-1-3-23(34-25(38)9-14-36-28(41)6-7-29(36)42)31(45)33-12-16-47-18-20-49-22-21-48-19-17-46-15-10-30(43)44/h4-7,23H,1-3,8-22H2,(H,32,37)(H,33,45)(H,34,38)(H,43,44)
SMILES
C1=CC(=O)N(C1=O)CCC(=O)NCCCCC(C(=O)NCCOCCOCCOCCOCCC(=O)O)NC(=O)CCN2C(=O)C=CC2=O

Bis-Mal-Lysine-PEG4-acid, is designed to provide a flexible, water-compatible spacer that can connect two functional handles for multivalent PROTAC assembly. Its PEG-based architecture supports favorable solubility and conformational adaptability, while the maleyl-lysine motif enables controlled conjugation strategies commonly used in targeted protein degradation workflows. The

Structure: The linker contains a PEG4-derived hydrophilic segment that imparts flexibility and aqueous compatibility, flanked by bis-maleimide-reactive lysine-derived functionalities and a terminal carboxylic acid for handle-based coupling. It features amide and ether linkages, with maleimide-type electrophilic centers suitable for selective thio-conjugation.

Reactivity: Suitable PROTAC construction typically relies on thiol–maleimide conjugation under mild, near-neutral conditions to form stable thioether linkages. Reaction progress is commonly monitored by analytical methods, with careful control of thiol equivalents and pH to maintain maleimide reactivity while minimizing side reactions such as hydrolysis. Water-miscible buffers and compatible organic co-solvents are often used, and inert atmosphere is sometimes employed to limit thiol oxidation.

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It is commonly abbreviated as: C1V1 = C2V2

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Tip: Chemical formula is case sensitive. C22H30N4O c22h30n40
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