| Bioactivity | 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]. | ||||||||||||
| Target | IC50: ~70 nM (CAR) | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | CINPA1 | ||||||||||||
| CAS | 102636-74-8 | ||||||||||||
| Formula | C23H29N3O3 | ||||||||||||
| Molar Mass | 395.49 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Cherian MT, et al. CINPA1 is an inhibitor of constitutive androstane receptor that does not activate pregnane X receptor. Mol Pharmacol. 2015 May;87(5):878-89. |