Bcl-2-IN-9

Bcl-2-IN-9 is a novel proapoptotic Bcl-2 inhibitor with IC50 value of 2.9 μM and low cytotoxic. Bcl-2-IN-9 mediates apoptosis by down-regulating expression of Bcl-2 in cancer cells and has a high selectivity against leukemia cells[1].

Signaling Pathways >> Apoptosis >> Bcl-2 Family

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Bcl-2:2.9 μM (IC50, [1])

Bcl-2-IN-9 (compound 6e) (10 μM, 48 hours) inhibits HL-60 cells in vitro[1]. Bcl-2-IN-9 (compound 6e) (10 μM, 48 hours) shows low cytotoxic effects against WI-38 cells with cell viability of 91%[1]. Bcl-2-IN-9 (compound 6e) (10 μM, 48 hours) displays a high selectivity against leukemia cells[1]. Bcl-2-IN-9 (compound 6e) (10 μM) mediates apoptotic by down-regulating expression of Bcl-2 and causing chromatin compaction and nuclear fragmentation[1]. Cell Viability Assay[1] Cell Line: HL-60 cells Concentration: 1, 10, 20, 40 μM Incubation Time: 48 hours Result: Surpressed cell growth and viability to 28.9%. Cell Cytotoxicity Assay[1] Cell Line: WT-38 cells Concentration: 10 μM Incubation Time: 48 hours Result: Low cytotoxic effects. Apoptosis Analysis[1] Cell Line: HL-60 cells Concentration: 1, 10, 20, 40 μM Incubation Time: 48 hours Result: Caused chromatin compaction and nuclear fragmentation.

[1]. Yukari Ono, et al. Design and synthesis of quinoxaline-1,3,4-oxadiazole hybrid derivatives as potent inhibitors of the anti-apoptotic Bcl-2 protein. Bioorg Chem. 2020 Aug; 104: 104245.