GeneBLAzer™ RARγ-UAS-bla HEK 293T Cells

The GeneBLAzer™ RAR gamma-UAS-bla HEK 293T cells contain the ligand binding domain (LBD) of the human retinoic acid receptor gamma (RAR gamma) fused to the DNA-binding domain of GAL4, stably integrated in the GeneBLAzer™ UAS-bla HEK 293T cell line. GeneBLAzer™ UAS-bla HEK 293T cells (Cat. No. K1104) stably express a beta-lactamase reporter gene under the transcriptional control of an upstream activator sequence (UAS). When an agonist binds to the LBD of the GAL4 (DBD)-RAR gamma (LBD) fusion protein, it binds to the UAS, inducing transcription of beta-lactamase. GeneBLAzer™ RAR gamma-UAS-bla HEK 293T cells have been tested for assay performance using variable assay conditions, including DMSO concentration, cell number, stimulation time, and substrate loading time. The Z' and EC50 concentrations of all-trans-retinoic acid and other stimuli have been determined. Additional testing data are available upon request.

RAR gamma is a member of the retinoic acid receptor family of nuclear receptors. Retinoids, vitamin A and its natural and synthetic analogues, are a very important group of hormones that regulate a wide variety of biological functions including embryogenesis, cell growth, and cell differentiation. Retinoids are beneficial in a wide variety of clinical cases including dermatology, oncology, diabetes, and diseases associated with HPV. RAR gamma is the predominant RAR subtype present in the skin and it constitutes more than 90% of the total skin or keratinocyte RAR repertoire. Skin irritation is a classical toxicity associated with RAR pan-agonists, like RA or TTNPB, and is believed to be a manifestation of RAR gamma activation. Furthermore, it has been shown that tumor-specific apoptosis can be driven by RAR gamma selective agonists, for pancreatic cancer cells.