4-[(8-Aminooctyl)amino]-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione HCl

Description

Thalidomide-NH-C8-NH2 is a Thalidomide -based cereblon ligand with a linker, which is a useful precursor for synthesis of PROTAC degraders. Targeted protein degradation (TPD) is an emerging therapeutic modality with the potential to tackle disease-causing proteins that have historically been highly challenging to target with conventional small molecules. PROTAC degraders are usually heterobifunctional small molecules consisting of two ligands joined by a linker: one ligand recruits and binds a protein of interest (POI) while the other recruits and binds an E3 ubiquitin ligase. Simultaneous binding of the POI and ligase by the PROTAC induces ubiquitylation of the POI and its subsequent degradation by the ubiquitin–proteasome system (UPS), after which the PROTAC is recycled to target another copy of the POI.

Uses

Thalidomide-NH-C8-NH2 is a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker used in PROTAC technology[1].

IC 50

Cereblon

References

[1] Sato T, et al. Cereblon-Based Small-Molecule Compounds to Control Neural Stem Cell Proliferation in Regenerative Medicine.Front Cell Dev Biol. 2021;9:629326. Published 2021 Mar 11. DOI:10.3389/fcell.2021.629326
[2] Nalawansha DA, et al. PROTACs: An Emerging Therapeutic Modality in Precision Medicine. Cell Chem Biol. 2020;27(8):998-985. DOI:10.7554/eLife.57277