BRD4 Inhibitor-18

BRD4 Inhibitor-18 is a highly potent BRD4 inhibitor with IC50 value of 110 nM. BRD4 Inhibitor-18 has a hydrophobic acetylcyclopentanyl side chain. BRD4 Inhibitor-18 can significantly suppress the proliferation of MV-4-11 cells with high BRD4 level. BRD4 Inhibitor-18 has apoptosis-promoting and G0/G1 cycle-arresting activity[1].

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> c-Myc

Signaling Pathways >> Epigenetics >> Epigenetic Reader Domain

IC50: 110 nM (BRD4)[1]

BRD4 Inhibitor-18 (compound 13f) (0-10 μM; 72 hours) can suppress the proliferation of HL-60 and MV-41 cells[1]. BRD4 Inhibitor-18 (0.5 and 5 μM; 12 hours) significantly arrests MV-4-11 cells in G1 phase in a dose-dependent manner[1]. BRD4 Inhibitor-18 (0.5 and 5 μM; 12 hours) effectively induces apoptosis of MV-4-11 cells in a dose-dependent manner[1]. BRD4 Inhibitor-18 (0.5 and 5 μM; 4 hours) inhibits the expression of c-Myc protein in a dose-dependent manner[1]. Cell Proliferation Assay Cell Line: HL-60 and MV-4-11[1] Concentration: 0-10 μM Incubation Time: 72 hours Result: Suppressed the proliferation of HL-60 and MV-41 cells with IC50s of 5.52 μM and 0.42 μM. Cell Cycle Analysis Cell Line: MV-4-11 cells[1] Concentration: 0.5 and 5 μM Incubation Time: 12 hours Result: Significantly arrested MV-4-11 cells in G1 phase in a dose-dependent manner. Apoptosis Analysis Cell Line: MV-4-11 cells[1] Concentration: 0.5 and 5 μM Incubation Time: 12 hours Result: Effectively induced apoptosis of MV-4-11 cells in a dose-dependent manner. Western Blot Analysis Cell Line: MV-4-11 cells[1] Concentration: 0.5 and 5 μM Incubation Time: 4 hours Result: Inhibited the expression of c-Myc protein in a dose-dependent manner.

[1]. Li Q, Li J, Cai Y, et al. Design, synthesis and biological evaluation of novel 6-phenyl-1,3a,4,10b-tetrahydro-2H-benzo[c]thiazolo[4,5-e]azepin-2-one derivatives as potential BRD4 inhibitors. Bioorg Med Chem. 2020;28(15):115601.