Many non-steroidal anti-inflammatory drugs (NSAIDs) are potent but non-selective inhibitors of both COX-1 and COX-2 in humans.¹ Sulindac is one of the older NSAIDs, an isostere of indomethacin developed before the inducible form of cyclooxygenase (COX-2) was discovered.² Although a number of NSAIDs have been found to protect against digestive tract cancers, sulindac has an extensive epidemiology documenting reduced human colorectal cancer. In murine models, sulindac was found not only to inhibit the enzymatic activity of polyp-associated COX-2, but also to downregulate the expression of colonic COX-2 protein to control levels.³

1 Barnett, J., Chow, J., Ives, D., et al. Purification, characterization and selective inhibition of human prostaglandin G/H synthase 1 and 2 expressed in the baculovirus system. Biochim Biophys Acta 1209 130-139 (1994).

2 Shen, T., and Winter, C.A. Chemical and biological studies on indomethacin, sulindac, and their analogs. Adv Drug Res 12 89-98 (1977).

3 Boolbol, S.K., Dannenberg, A.J., Chadburn, A., et al. Cyclooxygenase-2 overexpression and tumor formation are blocked by sulindac in a murine model of familial adenomatous polyposis. Cancer Res 56 2556-2560 (1996).

Barnett, J., Chow, J., Ives, D., et al. Purification, characterization and selective inhibition of human prostaglandin G/H synthase 1 and 2 expressed in the baculovirus system. Biochim Biophys Acta 1209 130-139 (1994).

Boolbol, S.K., Dannenberg, A.J., Chadburn, A., et al. Cyclooxygenase-2 overexpression and tumor formation are blocked by sulindac in a murine model of familial adenomatous polyposis. Cancer Res 56 2556-2560 (1996).

Shen, T., and Winter, C.A. Chemical and biological studies on indomethacin, sulindac, and their analogs. Adv Drug Res 12 89-98 (1977).

Sulindac is available in the following screening library:

• Bio-active Lipid I Screening Library (96-Well)