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Introduction of 102636-74-8 :
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. IC50 & Target: IC50: ~70 nM (CAR)In Vitro: CINPA1 (1μM ; 24 hours) inhibits CAR-mediated transactivation without activating PXR in HepG2 cells. CINPA1 is a specific xenobiotic receptor inhibitor and has no cytotoxic effects up to 30 μM. CINPA1 inhibits CAR-mediated gene expression in primary human hepatocytes, where CAR is endogenously expressed. CINPA1 does not alter the protein levels or subcellular localization of CAR. CINPA1 increases corepressor and reduces coactivator interaction with the CAR ligand-binding domain in mammalian two-hybrid assays. CINPA1 disrupts CAR binding to the promoter regions of target genes in chromatin immunoprecipitation assays. CINPA1 efficiently inhibits CAR-LBD interaction with the coactivator peptide that suggesting that CINPA1 is a ligand of CAR.