2585561-49-3

PROTAC BRD4 Degrader-17 (compound 13i) is a potent PROTAC BRD4 Degrader, with IC50 values of 29.54 nM (BRD4 (BD1)) and 3.82 nM (BRD4 (BD2)). PROTAC BRD4 Degrader-17 significantly attenuates G2/M progression associated Cyclin B1 expression. PROTAC BRD4 Degrader-17 significantly induces apoptosis in MV-4-11 cells[1].

BRD4 (BD2): 3.82 ± 0.0 nM (IC₅₀); BRD4 (BD1): 29.54 ± 2. nM (IC₅₀)

[1] Chen J, et al. Adjusted degradation of BRD4 S and BRD4 L based on fine structural modifications of the pyrrolopyridone scaffold. Eur J Med Chem. 2022 Jun 5;236:114259. DOI:10.1016/j.ejmech.2022.114259