E3 Ligase Ligand-Linker Conjugates 19

Thalidomide-O-acetamido-C4-amine HCl salt is comprised of a Thalidomide based cereblon ligand and a ligand-linker conjugate. This E3 ligase ligand-linker conjugate is used in PROTAC technology.

Thalidomide-O-amido-C4-NH2 (Cereblon Ligand-Linker Conjugates 6), a synthesized E3 ligase ligand-linker conjugate that incorporates the Thalidomide based cereblon ligand and a linker, can be used in the synthesis of PROTACs[1].

Cereblon

[1] Zhou B, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins withPicomolar Cellular Potencies and Capable of Achieving Tumor Regression.J Med Chem. 2018 Jan 25;61(2):462-481. DOI:10.1021/acs.jmedchem.6b01816
[2] James Bradner, et al. Methods to induce targeted protein degradation through bifunctional molecules. WO 2017024317 A2.