Apoptotic agent-2

Apoptotic agent-2 (compound 14b) induces apoptosis by down-regulation of Bcl-2 and up-regulation of Bax and caspase-3. Apoptotic agent-2 exhibits anti-proliferative activities and can be used for cancer research[1].

Signaling Pathways >> Apoptosis >> Bcl-2 Family

Signaling Pathways >> Apoptosis >> Apoptosis

Research Areas >> Cancer

Signaling Pathways >> Apoptosis >> Caspase

Bax

Caspase 3

Bcl-2

Apoptotic agent-2 (compound 14b) (24 hours) has selective anti-proliferative activities against HCT-116, HepG-2, MCF-7 and WI-38 (normal human cells) cells with IC50 values of 1.96, 1.12, 2.38 and 107.5 µM, respectively[1]. Apoptotic agent-2 (compound 14b) (1.12 μM; 24 hours; HepG-2 cells) induces cell apoptosis, which increases the levels of active Caspase-3 and BAX by 10.92 folds and 9.7 folds, respectively, and decreases the level of Bcl-2 by 3.3 folds[1]. Cell Cycle Analysis[1] Cell Line: HepG-2 cells Concentration: 1.12 μM Incubation Time: 24 hours Result: The percentage of cells in the G2-M phase increased while the percentage of cells in G0-G1 phase and S phase decreased. Apoptosis Analysis[1] Cell Line: HepG-2 cells Concentration: 1.12 μM Incubation Time: 24 hours Result: Increased the early apoptosis ratio from 0.69% to 5.17% and increased the late apoptosis ratio from 0.32% to 12.11%.

[1]. Fayed EA, et al. In vitro cytotoxic activity of thiazole-indenoquinoxaline hybrids as apoptotic agents, design, synthesis, physicochemical and pharmacokinetic studies. Bioorg Chem. 2020 Jul;100:103951.