4-(3-azidopropoxy)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione Usage And Synthesis

Uses

Thalidomide-O-C3-azide is a click chemistry modification of the cereblon (CRBN) inhibitor Thalidomide (HY-14658). Thalidomide-O-C3-azide contains an azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing alkyne groups. Thalidomide-O-C3-azide can be used as a ligand of E3 ubiquitin ligase and Linker conjugates (E3 Ligase Ligand-Linker Conjugates) for the synthesis of PROTACs[1].

Biological Activity

Thalidomide 4'-ether-alkylC3-azide is a functionalized cereblon ligand for PROTAC? research and development; incorporates an E3 ligase ligand plus an alkylC3 linker with a terminal azide ready for conjugation to a target protein ligand.

storage

Store at -20°C

References

[1] Fischer ES, et al. Structure of the DDB1-CRBN E3 ubiquitin ligase in complex with thalidomide. Nature. 2014 Aug 7;512(7512):49-53. DOI:10.1038/nature13527

4-(3-azidopropoxy)-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione(2758432-00-5)Related Product Information

• Thalidomide-NH-C4-NH-Boc
• 2-(2,6-DIOXOPIPERIDIN-3-YL)-5-FLUORO-6-(PIPERAZIN-1-YL)ISOINDOLINE-1,3-DIONE HCL
• 2-(2,6-Dioxo-3-piperidinyl)-4-[2-[2-(2-propyn-1-yloxy)oxy]ethoxy]-1H-isoindole-1,3(2H)dione