CINPA 1

Modify Date: 2025-08-27 10:21:52

CINPA 1 Structure
CINPA 1 structure
Common Name CINPA 1
CAS Number 102636-74-8 Molecular Weight 395.49
Density N/A Boiling Point N/A
Molecular Formula C23H29N3O3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of CINPA 1


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].

 Names

Name CINPA1

 CINPA 1 Biological Activity

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].
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

[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.

 Chemical & Physical Properties

Molecular Formula C23H29N3O3
Molecular Weight 395.49
InChIKey AYQBYSPEGRYKFA-UHFFFAOYSA-N
SMILES CCOC(=O)Nc1ccc2c(c1)N(C(=O)CN(CC)CC)c1ccccc1CC2

 CINPA 1Bioassay

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Name: This assay (PMID: 37558952) monitors the impact of a chemical compound on general aut...
Source: ChEMBL
Target: TERT-RPE1
External Id: CHEMBL5724699
Name: Thermal Shift Assay. Domain: start/stop: N44-E168
Source: ChEMBL
Target: Bromodomain-containing protein 4
External Id: CHEMBL5060944
Name: Thermal Shift Assay. Domain start/stop: M626-G740
Source: ChEMBL
Target: Peregrin
External Id: CHEMBL4650107
Name: Thermal Shift Assay. Domain: start/stop: M1-L298
Source: ChEMBL
Target: Cyclin-dependent kinase 2
External Id: CHEMBL5062802
Name: Inverse agonist activity at GST tagged-human CAR-LBD assessed as reduction in fluores...
Source: ChEMBL
Target: Nuclear receptor subfamily 1 group I member 3
External Id: CHEMBL3767622
Name: SARS-CoV-2 3CL-Pro protease inhibition percentage at 20µM by FRET kind of response f...
Source: ChEMBL
Target: Replicase polyprotein 1ab
External Id: CHEMBL4495582
Name: Enzymatic assay of human HDAC6 with commercial peptide substrate
Source: ChEMBL
Target: Histone deacetylase 6
External Id: CHEMBL4808149
Name: Enzymatic assay of human HDAC6 with custom peptide substrate
Source: ChEMBL
Target: Histone deacetylase 6
External Id: CHEMBL4808150
Name: Thermal Shift Assay. Domain: start/stop: E122-S403
Source: ChEMBL
Target: Aurora kinase A
External Id: CHEMBL5067447
Name: High-throughput screen for inhibitors of the GIV GBA-motif interaction with Galpha-i ...
Source: ICCB-Longwood/NSRB Screening Facility, Harvard Medical School
External Id: HMS1303
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