CINPA 1 structure
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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 1CINPA1 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]. |
| Name | CINPA1 |
|---|
| 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 |
| InChIKey | AYQBYSPEGRYKFA-UHFFFAOYSA-N |
| SMILES | CCOC(=O)Nc1ccc2c(c1)N(C(=O)CN(CC)CC)c1ccccc1CC2 |
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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
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Name: Thermal Shift Assay. Domain: start/stop: N44-E168
Source: ChEMBL
Target: Bromodomain-containing protein 4
External Id: CHEMBL5060944
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Name: Thermal Shift Assay. Domain start/stop: M626-G740
Source: ChEMBL
Target: Peregrin
External Id: CHEMBL4650107
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Name: Thermal Shift Assay. Domain: start/stop: M1-L298
Source: ChEMBL
Target: Cyclin-dependent kinase 2
External Id: CHEMBL5062802
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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
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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
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Name: Enzymatic assay of human HDAC6 with commercial peptide substrate
Source: ChEMBL
Target: Histone deacetylase 6
External Id: CHEMBL4808149
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Name: Enzymatic assay of human HDAC6 with custom peptide substrate
Source: ChEMBL
Target: Histone deacetylase 6
External Id: CHEMBL4808150
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Name: Thermal Shift Assay. Domain: start/stop: E122-S403
Source: ChEMBL
Target: Aurora kinase A
External Id: CHEMBL5067447
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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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