Description: CITCO inhibits growth and expansion of brain tumour stem cells (BTSCs) and has an EC50 of 49 nM over pregnane X receptor (PXR), and no activity on other nuclear receptors. CITCO is an imidazothiazole derivative and it also is a selective Constitutive androstane receptor (CAR) agonist. Target: Apoptosis,...

CITCO is an agonist of human CAR (EC50 = 49 nM). It induces nuclear translocation of human CAR in hepatocytes, followed by increased expression of CAR-regulated genes, including several cytochrome P450 isoforms. CITCO less potently activates human pregnane X receptor (EC50 = 3 µM) and has no detectable activity on...