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CYP1A1 is an extrahepatic cytochrome P450 with broad substrate specificity involved in the metabolism of numerous potentially toxic and carcinogenic compounds. This cell-based assay measures CYP1A1 induction via the aryl hydrocarbon receptor (AhR) pathway. CYP1A1 induction is regulated by AhR, a transcription factor existing in a multiprotein complex in the cytoplasm. Ligands bind AhR in the cytoplasm of the cells, whereupon the AhR-ligand complex translocates to the nucleus and forms a heterodimer with AhR nuclear translocator (Arnt). This complex then binds the dioxin response element (DRE) in the 5' upstream region of the CYP1A1 promoter, enhancing CYP1A1 expression.
The GeneBLAzer™ CYP1A1-bla LS-180 cell line contains a beta-lactamase reporter gene whose expression is driven by the CYP1A1 promoter, which serves as a readout for CYP1A1 expression. This cell line has been tested for assay performance under variable conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time. The Z' and EC50 concentrations of 2, 3, 7, 8- tetrachlorodibenzo-p-dioxin (TCDD) were determined. Other CYP1A1 inducers include synthetic and natural chemicals including halogenated and polycyclic aromatic hydrocarbons, and dietary compounds such as flavonoids. Additional testing information using known activators of the pathway are also provided. Academic and non-profit customers, please inquire for special pricing.