thalidomide 5 fluoride

Thalidomide 5-fluoride (H-Isoindole-1,3(2H)-dione, 2-(2,6-dioxo-3-piperidinyl)-5-fluoro-) is a thalidomide-based Cereblon ligand that binds to the IRAK4 protein ligand via a linker to form PROTACIRAK4 degrader-1.

Thalidomide-Piperazine 5-fluoride is a compound synthesized as an E3 ligase ligand-linker conjugate, incorporating a cereblon ligand derived from Thalidomide and utilizing a linker commonly employed in PROTAC technology.

Thalidomide-Piperazine 5-fluoride hydrochloride, a derivative of the cereblon (CRBN) inhibitor Thalidomide, serves as a ligand for E3 ubiquitin ligase (Ligands for E3 Ligase), facilitating the synthesis of PROTACs [1].

JMV7048 is an effective PROTAC degrader targeting the PXR (Pregnane X Receptor), with a DC50 of 379 nM. It induces the polyubiquitination and degradation of PXR protein by recruiting the E3 CRBN ubiquitin ligase and the 26S proteasome. This degradation of PXR significantly enhances the chemosensitivity of colorectal cancer stem cells, substantially delaying cancer recurrence in vivo. The composition of JMV7048 includes the PXR agonist JMV6944, a linker, and Thalidomide 5-fluoride.