Rosbin, a synthetic small molecule, induces A549 cells apoptosis through a ROS‐mediated pathway

Rosbin (Thieno [2, 3‐c] piperidine‐3‐carboxamide‐2‐[(3‐methoxy‐naphtha‐lene‐2‐carbonyl)‐amino]‐6‐(benzyl)‐, hydrochloride), a synthetic piperidinothieno derivative compound obtained from chemical genetics screenings, significantly suppresses the viability of non‐small cell lung cancer A549 cells with an IC50 of 2.05 ± 0.31 µM. It only decreases growth of non‐tumour MRC‐5 cells at the doses higher than 10 µM. Rosbin induces apoptosis in a dose‐dependent manner by reducing the mitochondrial membrane potential (MMP) and increasing activities of caspases‐3/7 and caspase‐9 in A549 cells, without affecting the activity of caspase‐8. Further studies showed that reactive oxygen species (ROS) induced apoptosis of A549 in the presence of rosbin as apoptosis was inhibited by N‐acetyl cysteine (NAC). These results suggest that rosbin is a novel apoptosis inducer, and ROS played a significant role in the A549 apoptosis induced by rosbin.