product name CH-223191
Description: CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 NM. It can prevent 2,3,7,8-TCDD-induced toxicity by antagonizing the aryl hydrocarbon receptor. In addition, CH-223191 blocked the binding of TCDD to AhR and inhibited TCDD-mediated nuclear translocation and DNA binding of AhR. These inhibitory effects of CH-223191 prevented the expression of cytochrome P450 enzymes, target genes of the AhR.
References: Mol Pharmacol. 2006 Jun;69(6):1871-8; Oncogene. 2009 Jul 16;28(28):2593-605.
333.39
Formula
C19H19N5O
CAS No.
301326-22-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 66 mg/mL (198.0 mM)
Water: <1 mg/mL
Ethanol: 4 mg/mL (12.0 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19393117
| In Vitro |
In vitro activity: CH-223191 blocks TCDD-mediated nuclear translocation and DNA binding of AhR, and also causes the inhibition of TCDD-induced cytochrome P450 enzyme activity. In human glioblastoma cells, CH-223191downregulates the TGF-beta/Smad pathway, and reduces clonogenic survival and invasiveness. In SK-N-SH human-derived neuronal cells, CH223191 counteracts the TCDD-induced suppression of neuronal acetylcholinesterase expression. In endothelial cells, CH-223191 potentiates ICAM-1 expression and prevents RelB nuclear translocation. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | CH-223191 (10 mg/kg/day, p.o.) potently prevents TCDD-caused cytochrome P450 induction, liver toxicity, and wasting syndrome in mice. |
| Animal model | Male ICR mice |
| Formulation & Dosage | Dissolved in Coin oil; 10 mg/kg; p.o. |
| References | Mol Pharmacol. 2006 Jun;69(6):1871-8; Oncogene. 2009 Jul 16;28(28):2593-605. |
Related Posts
product name CH-223191
Description: CH-223191 is a potent and specific aryl hydrocarbon receptor (AhR) antagonist with IC50 of 30 NM. It can prevent 2,3,7,8-TCDD-induced toxicity by antagonizing the aryl hydrocarbon receptor. In addition, CH-223191 blocked the binding of TCDD to AhR and inhibited TCDD-mediated nuclear translocation and DNA binding of AhR. These inhibitory effects of CH-223191 prevented the expression of cytochrome P450 enzymes, target genes of the AhR.
References: Mol Pharmacol. 2006 Jun;69(6):1871-8; Oncogene. 2009 Jul 16;28(28):2593-605.
333.39
Formula
C19H19N5O
CAS No.
301326-22-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 66 mg/mL (198.0 mM)
Water: <1 mg/mL
Ethanol: 4 mg/mL (12.0 mM)
Solubility (In vivo)
Synonyms
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19393117
| In Vitro |
In vitro activity: CH-223191 blocks TCDD-mediated nuclear translocation and DNA binding of AhR, and also causes the inhibition of TCDD-induced cytochrome P450 enzyme activity. In human glioblastoma cells, CH-223191downregulates the TGF-beta/Smad pathway, and reduces clonogenic survival and invasiveness. In SK-N-SH human-derived neuronal cells, CH223191 counteracts the TCDD-induced suppression of neuronal acetylcholinesterase expression. In endothelial cells, CH-223191 potentiates ICAM-1 expression and prevents RelB nuclear translocation. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | CH-223191 (10 mg/kg/day, p.o.) potently prevents TCDD-caused cytochrome P450 induction, liver toxicity, and wasting syndrome in mice. |
| Animal model | Male ICR mice |
| Formulation & Dosage | Dissolved in Coin oil; 10 mg/kg; p.o. |
| References | Mol Pharmacol. 2006 Jun;69(6):1871-8; Oncogene. 2009 Jul 16;28(28):2593-605. |