CAY10404 (3-(4-METHYLSULPHONYLPHENYL)-4-PHENYL-5-T) is a potent and highly selective inhibitor of COX-2 and COX-1. It is also a potent inhibitor of PKB/Akt and MAPK signalling pathways and induces apoptosis in NSC-LC cells, with analgesic, anti-inflammatory and anti-cancer activities.

COX-2:1 nM, COX-1:>500 μM

CAY10404处理（在10-100μM范围内）导致剂量依赖性的细胞生长抑制，平均50%抑制浓度（IC(50)）为60-100μM/升，具体取决于细胞系。西部印迹分析显示，CAY10404处理的细胞中poly (ADP-ribose) polymerase （PARP）和procaspase-3发生裂解，这表明caspase活性和细胞凋亡的发生。CAY10404处理在H460和H358细胞中抑制了Akt、糖原合酶激酶-3β和细胞外信号调节激酶1/2的磷酸化[1]。

To measure the effects of CAY10404 on proliferation of NSCLC cells, 3 x 10(3) cells/well were plated in 96-well plates and allowed to adhere overnight at 37 degrees C. After treatment with CAY10404 for 3 days, cell proliferation was measured by the 3- (4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) assay. In the H460 NSCLC cells, evidence of apoptosis was sought using the terminal deoxynucleotidyl transferase deoxyuridine triphosphate (dUTP) nick end labelling (TUNEL) assay and western blot analysis[1].