The HTR2B Knockout HL-60 Cell Line is a CRISPR/Cas9-edited knockout model that disrupts the HTR2B gene, encoding the 5-HT2B serotonin receptor. Derived from the human promyelocytic leukemia cell line HL-60, this stable loss-of-function tool enables detailed investigation of serotonin receptor-mediated signaling in leukemia biology. This knockout cell line provides a critical platform for exploring serotonin-dependent processes in leukemic cells, including proliferation and differentiation.
HL-60 cells are a well-characterized human promyelocytic leukemia line, originally derived from a patient with acute promyelocytic leukemia. They are extensively employed to study the molecular mechanisms governing myeloid differentiation, cell cycle regulation, and apoptosis. Their ability to differentiate into macrophage- or neutrophil-like cells upon chemical induction makes them a versatile model for hematopoietic research.
HTR2B is a G protein-coupled receptor that, upon serotonin (5-HT) binding, activates G??q/11. This stimulates phospholipase C-?? (PLC-??), generating IP3 and DAG, which mobilize intracellular Ca2+ and activate protein kinase C (PKC). Downstream, the MAPK/ERK cascade is engaged, with ERK1/2 phosphorylating transcription factors FOS and JUN. ??-arrestin also interacts with the receptor to modulate signaling. The core pathway includes HTR2B, GNAQ, PLCB1, PRKCA, and MAPK1.
In HL-60 cells, serotonin/HTR2B signaling influences proliferation and survival, though precise roles remain undefined. Knockout of HTR2B eliminates serotonin-induced calcium transients and MAPK activation, providing a clean background to study receptor-specific effects. This model is pertinent for investigating acute myeloid leukemia pathology and links to HTR2B-associated disorders such as valvular heart disease, pulmonary hypertension, and fibrosis.
Researchers can leverage the HTR2B Knockout HL-60 Cell Line to perform quantitative calcium mobilization assays using Fluo-4 fluorescence, directly assessing receptor-mediated intracellular Ca2+ dynamics. Phospho-ERK ELISA or western blotting enables precise measurement of MAPK/ERK pathway activation, while MTT colorimetric assays quantify changes in cellular proliferation and viability. Flow cytometry facilitates multi-parametric analysis of differentiation markers and cell cycle distribution. Additionally, transwell migration assays can evaluate the receptor??s role in motility, and co-culture setups can dissect serotonin-dependent immune cell interactions. For technical support or licensing inquiries, please contact Ascent Research.
