The HRH1 Knockout UM-UC-3 Polyclonal Cells constitute a CRISPR/Cas9-edited polyclonal knockout cell population targeting the human HRH1 gene. This product provides a heterogeneous pool of UM-UC-3 cells with disrupted HRH1 expression, enabling loss-of-function studies in a transitional cell carcinoma background. As a polyclonal knockout model, it is designed for robust functional genomics research without clonal isolation, allowing direct examination of histamine H1 receptor-dependent signaling in bladder cancer cells.
The UM-UC-3 cell line is a widely used human bladder cancer model derived from a male patient with transitional cell carcinoma. It serves as a representative urothelial cancer epithelial line, exhibiting characteristic features of high-grade bladder tumors. These cells are amenable to a variety of cellular assays, including proliferation, migration, and chemotaxis studies, making them a suitable host for investigating HRH1-mediated processes in a cancer-relevant context.
The HRH1 gene encodes the histamine H1 receptor, a Gq/11-coupled receptor that mediates histamine signals. Upon activation, G??q/11 stimulates phospholipase C (PLCB), generating IP3 and DAG. IP3 triggers calcium release via ITPR channels, while DAG activates protein kinase C (PRKCA). Downstream, NF-??B and MAPK pathways regulate inflammatory and proliferative genes. Receptor desensitization involves GRK2 phosphorylation, ??-arrestin binding, and clathrin-mediated endocytosis. Pharmacological agents like cetirizine and fexofenadine serve as upstream regulators.
In UM-UC-3 cells, HRH1 knockout abolishes histamine-evoked Gq/11 signaling, disrupting calcium flux and downstream effectors. This model dissects histamine??s role in urothelial carcinoma, including inflammation, cell motility, and proliferation. It isolates HRH1-specific effects from other histamine receptors and facilitates evaluation of H1 receptor blockade in bladder cancer, while enabling study of crosstalk with oncogenic pathways.
This polyclonal knockout pool suits applications in receptor pharmacology, cancer signaling, and drug screening. Representative assays include calcium flux measurement, phospho-PKC western blot, RT-qPCR for NF-??B targets, and functional assays such as migration and histamine-induced proliferation. The polyclonal format enables population-level analyses. For further information, contact Ascent Research.
