CAY10404

CAY10404 is a potent and selective cyclooxygenase-2 (COX-2) inhibitor with an IC₅₀ of 1 nM and a selectivity index (SI; COX-1 IC₅₀/COX-2 IC₅₀) of >500000. CAY10404 is a potent PKB/Akt and MAPK signaling pathways inhibitor and induces apoptosis in non-small cell lung cancer (NSCLC) cells. CAY10404, a diarylisoxazole, has good analgesic, anti-inflammatory, and anti-cancer activities^[1][2][3]. In Vitro: CAY10404 (compound 7) exhibits no inhibition of COX-1 (IC₅₀>500 µM)^[1].
CAY10404 (10-100 µM; for 3 days) inhibits the growth of NSCLC cell lines in a concentration-dependent manner and has an average 50% inhibitory concentration (IC₅₀) of 60-100 µM^[3].
CAY10404 (20-100 µM; for 3 days) induces apoptosis in NSCLC cells^[3].
CAY10404 (80 µM; for 3 days) induces a concentration-dependent decrease in the level of the anti-apoptotic proteins (Bcl-2 and Bcl-X_L) and pAkt and pGSK-3β^[3].
CAY10404 (20, 50, 80, 100 µM; for 14 days) compromises the ability of H460 cells to form colonies in anchorage-independent growth in a concentration-dependent manner^[3].
In Vivo: CAY10404 (50 mg/kg/day; ip; for 4 days) decreases lung inflammation in HTV mice and attenuates ventilator-induced lung injury^[2].