| Name | CINPA1 |
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| Description | 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]. |
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| Related Catalog | |
| 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]. |
| References |
| Molecular Formula | C23H29N3O3 |
|---|---|
| Molecular Weight | 395.49 |