tcsc0569 Sulindac

Sulindac is a non-steroidal antiinflammatory agent, acts as a COX-2 inhibitor, and inhibits overexpression of COX-2.

IC50 & Target: COX-2^[1]

In Vitro: Sulindac is a non-steroidal antiinflammatory agent, acts as a COX-2 inhibitor, and inhibits overexpression of COX-2^[1]. Sulindac (0.1 mM to 0.5 mM) causes limited death in both p53 wt and p53 null HCT116 cells, but in combination with vitamin C, it dramatically increases almost 5-fold in cell death in p53 wt HCT116 cells relative to the vitamin C alone, and such an effect is involving caspase activation and p53 function in these cells, and via ROS-mediated pathway. Sulindac combined with vitamin C significantly increases PUMA levels, but shows no effect on Bim, Bcl-2 and Mcl-1 levels^[2]. Sulindac (500 μM) in combination with celecoxib blocks transforming growth factor (TGF)-β1-induced epithelial-mesenchymal transition, migration and invasion in A549 cells. The combination also suppresses involvement of sirtuin 1 (SIRT1) in transforming growth factor (TGF)-β1-induced epithelial-mesenchymal transition (EMT)^[3].

In Vivo: Sulindac (0.5 ± 0.1 mg/day) decreases COX, modolates PGE2 levels and prevents tumor formation in the Min mice^[1].