CINPA1 is a potent and specific inhibitor of constitutive androstane receptor (CAR) that does not activate pregnane X receptor (PXR). CINPA1 reduces CAR-mediated transcription with an IC₅₀ of ~70 nM. CINPA1 can be used as a molecular tool for understanding CAR function^[1]. IC50 & Target: IC50: ~70 nM (CAR)^[1] In Vitro: CINPA1 (1μM ; 24 hours) inhibits CAR-mediated transactivation without activating PXR in HepG2 cells^[1].
CINPA1 is a specific xenobiotic receptor inhibitor and has no cytotoxic effects up to 30 μM^[1].
CINPA1 inhibits CAR-mediated gene expression in primary human hepatocytes, where CAR is endogenously expressed^[1].
CINPA1 does not alter the protein levels or subcellular localization of CAR^[1].
CINPA1 increases corepressor and reduces coactivator interaction with the CAR ligand-binding domain in mammalian two-hybrid assays^[1].
CINPA1 disrupts CAR binding to the promoter regions of target genes in chromatin immunoprecipitation assays^[1].
CINPA1 efficiently inhibits CAR-LBD interaction with the coactivator peptide that suggesting that CINPA1 is a ligand of CAR^[1].