Bis-Propargyl-PEG13

Description

Bis-propargyl-PEG13 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs.

Uses

Bis-propargyl-PEG12 is a PEG-based PROTAC linker that can be used in the synthesis of PROTACs[1]. Bis-propargyl-PEG12 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

in vitro

PROTACs contain two different ligands connected by a linker; one is a ligand for an E3 ubiquitin ligase and the other is for the target protein. PROTACs exploit the intracellular ubiquitin-proteasome system to selectively degrade target proteins.

IC 50

PEGs

structure and hydrogen bonding

Bis-propargyl-PEG13 comprises two propargyl groups which can form triazole linkages with azide-bearing compounds or biomolecules in copper catalyzed Click Chemistry reactions. The hydrophilic PEG units help improve the solubility of the molecule in aqueous media.

References

[1] An S, et al. Small-molecule PROTACs: An emerging and promising approach for the development of targeted therapy drugs. EBioMedicine. 2018 Oct;36:553-562 DOI:10.1016/j.ebiom.2018.09.005