Rosiglitazone is an agonist of peroxisome proliferator-activated receptor gamma (PPARgamma). It activates PPARgamma1 and PPARgamma2 in reporter assays (EC50s = 30 and 100 nM, respectively). Rosiglitazone selectively activates chimeras containing the ligand-binding domains (LBDs) of PPARgamma over PPARalpha and...

AM80 is a retinoic acid receptor agonist that is selective for RARalpha (Kd = 62 nM, AC50 = 1.46 nM) compared to RARbeta (Kd = 280 nM, AC50 = 6.87 nM) and RARgamma (Kd = 816 nM, AC50 = 148.7 nM). It demonstrates greater specific binding to RARalpha compared to retinoic acid (Cay-11017), which exhibits little...

Liproxstatin-1 is a ferroptosis inhibitor. It inhibits ferroptotic cell death (IC50 = 22 nM) and lipid peroxidation in mouse embryonic fibroblasts (MEFs) with an inducible knockdown of glutathione peroxidase 4 (Gpx4-/- MEFs) when used at a concentration of 50 nM. Liproxstatin-1 also inhibits ferroptosis induced by...

STF-083010 is an inhibitor of the IRE1/XBP1 pathway, blocking IRE1 endonuclease activity without affecting its kinase activity after endoplasmic reticulum (ER) stress both in vitro and in vivo. STF-083010 (60 µM) reduces the splicing of XBP1 by IRE1 in the presence of thapsigargin (Cay-10522), an ER stress inducer....

Phenprocoumon is an anticoagulant and vitamin K antagonist. It inhibits the activity of wild-type vitamin K epoxide reductase (VKOR, IC50 = 4.2 nM), as well as a variety of mutant VKORs (IC50s = 5.1-835 nM), in cell-based reporter assays. Phenprocoumon inhibits prothrombin complex synthesis in rats in a...