PROTAC® composed of the BRD9 inhibitor BI 7273 conjugated to the cereblon E3 ligase ligand pomalidomide . Potent and selective degrader of BRD9 (IC50 = 56.6 nM in MOLM-13 cells). Does not degrade BRD4 or BRD7 at concentrations up to 5 μM. Displays antiproliferative effects in human AML cell lines. PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Remillard et al (2017) Degradation of the BAF complex factor BRD9 by heterobifunctional ligands. Angew.Chem.Int.Ed.Engl. 56 5738 PMID:28418626