Sulindac Sulfone (CAS 59864-04-9)

Sulindac Sulfone is a metabolite of Sulindac (sc-202823) which inhibits cell growth and induces apoptosis in human cancer cell lines. It does not, however, inhibit cyclooxygenase (Cox). In mouse models, sulindac not only inhibits the enzymatic activity of COX-2 associated with polyps, but also reduces the expression of colonic COX-2 protein to normal levels. Sulindac sulfone, an oxidized metabolite found in many mammals but minimally in mice and rats, is generally considered inactive against COX enzymes. In vitro, sulindac sulfone inhibits aldose reductase, with an IC50 of 367 nM, and this may contribute to the beneficial effects of sulindac on complications associated with type 2 diabetes. Sulindac sulfone acts as a growth inhibitor and inducer of apoptosis in cancer cell lines. It inhibits cell growth and induces apoptosis independently of cyclooxygenase inhibition, making it effective in inhibiting the development and inducing regression of premalignant adenomatous polyps. It also serves as a lipoxygenase and COX-2 inhibitor. Sulindac sulfone is classified as a cyclooxygenase 2 inhibitor, an EC 1.13.11.34 (arachidonate 5-lipoxygenase) inhibitor, and an apoptosis inducer. Chemically, it is a sulfone, a monocarboxylic acid, and an organofluorine compound. Its origin can be traced back to sulindac.