DC-BPi-11

DC-BPi-11 is an inhibitor of bromodomain PHD finger transcription factor (BPTF), with an IC50 value of 698 nM. DC-BPi-11 shows remarkable inhibition against leukemia cell proliferation[1].

Research Areas >> Cancer

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

698 nM (BPTF)[1]

DC-BPi-11 (0.1 nM-1 μM; 24 h) inhibits BPTF in human leukemia MV-4-11 cells with an EC50 value of 120 nM[1]. DC-BPi-11 (0.01 μM-100 μM; 24 h) significantly inhibits the proliferation of human leukemia MV-4-11 cells (IC50=0.89 μM), and (2.5-20 μM; 24 h) decreases downstream oncogene expression[1]. DC-BPi-11 (0.6-50 μM; 24 h) dose-dependently decreases c-Myc protein level[1]. DC-BPi-11 is safety and shows minimal effects on normal cells[1]. Western Blot Analysis[1] Cell Line: Human leukemia MV-4-11 cells Concentration: 0.6 μM, 1.8 μM, 5.6 μM, 16.6 μM, and 50 μM Incubation Time: 24 hours Result: Resulted depletion of c-Myc in a dose-dependent manner. Apoptosis Analysis[1] Cell Line: Human leukemia MV-4-11 cells Concentration: 5 μM, 10 μM, 20 μM Incubation Time: 24 hours Result: Induced cell apoptosis by arresting cell cycle at G1 phase.

[1]. Lu T, et al. Discovery of High-Affinity Inhibitors of the BPTF Bromodomain. J Med Chem. 2021 Aug 26;64(16):12075-12088.