AGN 193109

AGN 193109, a retinoid analog, is a potent and specific antagonist of RARs (Kds: 2 nM, 2 nM, and 3 nM for RARα, RARβ, and RARγ) .AGN 193109 is completely RAR specific because it does not bind to or transactivate through any of the RXRs . AGN 193109 (100 nM) inhibits the TTNPB (a retinoic acid receptor agonist) -dependent morphological change in ECE16-1 cells. AGN193109 half-reverses retinoid-dependent growth suppression at 10 nM, and completely shows this effect at 100 nM in ECE16-1 cells. AGN193109 (100 nM) also eliminates TTNPB-induced decrease in levels of K5, K6, K14, K16, and K17 and increases in levels of K7, K8, and K19 .AGN 193109 (0.30 or 1.20 μmol/kg) by topical treatment significantly reduces both weight loss and cutaneous toxicity caused by oral TTNPB cotreatment. AGN 193109 (1.15 μmol/kg) does not cause overt toxicity and has no effect on spleen weight on the mice, but it suppresses TTNPB-induced increase in spleen weight of the mice. AGN 193109 also significantly reduces the cutaneous toxicity induced by ATRA. (In Vitro) :AGN 193109 (0.1 and 1 μmol/L; 3 w) dose-dependently increases vascular smooth muscle cells (VSMCs) mineralization.AGN 193109 (100 nM; 10 d) induces human pluripotent stem cells (hPSCs) differentiate into olfactory placode cells and neurons.