Ro 41-5253

Ro 41-5253 is a selective retinoic acid receptor alpha (RARα) antagonist originally developed by Hoffmann-La Roche. It binds to RARα with high affinity (IC50 of approximately 60 nM) without inducing transcriptional activation or affecting RAR/RXR heterodimerization and DNA binding. Ro 41-5253 has been shown to inhibit cancer cell proliferation and induce apoptosis in various cancer cell lines, particularly estrogen receptor-positive breast cancer cells, and has demonstrated antitumor activity in preclinical models. Additionally, it acts as a partial agonist of peroxisome proliferator-activated receptor gamma (PPARγ).

Other names

4-[(1E)-2-[7-(heptyloxy)-3,4-dihydro-4,4-dimethyl-1,1-dioxido-2H-1-benzothiopyran-6-yl]-1-propen-1-yl]benzoic acid4-[(E)-2-(7-heptoxy-4,4-dimethyl-1,1-dioxo-2,3-dihydrothiochromen-6-yl)prop-1-enyl]benzoic acid4-[2-(7-(heptyloxy)-3,4-dihydro-4,4-dimethyl-2H-1-benzothiopyran-6-yl)-1-propenyl]benzoic acid S,S-dioxide