Key Features:
- High Sensitivity: The cell line offers high signal-to-background with over 100-fold induction in luciferase activity, ensuring accurate and reproducible results in CREB pathway studies.
- Sensitive and Quantitative: The luciferase reporter provides a direct and reliable readout of CREB activation, enabling precise measurement of pathway activity.
- Versatile Applications: Co-expression of GIPR and a CREB-responsive luciferase reporter mimics endogenous signaling cascades following GIPR activation. Suitable for screening applications and dose-response studies of GIPR-targeting compounds.
- Stable Integration: Established via co-transfection with GIPR and CRE-luciferase constructs, followed by antibiotic selection and functional screening with Tirzepatide.
The GIPR/CREB Luciferase Reporter HEK293 Stable Cell Line is derived from human embryonic kidney cells and stably expresses Gastric Inhibitory Polypeptide Receptor alongside a firefly luciferase reporter gene under the control of the cAMP response element-binding protein (CREB) response element. This dual-expression cell line is an ideal tool for monitoring the intracellular signaling events triggered by GIPR activation.
GIPR is a G protein-coupled receptor (GPCR) primarily coupled to the G proteins, leading to increased intracellular cAMP and subsequent activation of PKA and downstream effectors like CREB. Activation of CREB results in luciferase expression, offering a convenient and quantitative readout of pathway activation.
This cell line is ideal for studying GIPR agonists, screening for GPCR modulators, and investigating cAMP/PKA/CREB pathway dynamics. It is particularly useful for drug discovery programs targeting metabolic diseases, including type 2 diabetes and obesity.
This versatile cell line serves as a powerful in vitro tool for both basic research and translational applications in endocrinology, pharmacology, and metabolic disease research.
Customer Q&As:
Q1: What applications is this cell line best suited for?
The GIPR/CREB Stable HEK293 Cell Line is useful tool for GIPR agonist and antagonist screening, dual GLP-1/GIP drug discovery programs, potency and efficacy testing, mechanism-of-action studies and high-throughput screening (HTS) campaigns.
Q2: How does the assay work?
Upon ligand binding, GIPR activates the Gs–cAMP signaling pathway, leading to CREB activation. This drives expression of firefly luciferase, producing a bright luminescent signal directly proportional to receptor activity.
Q3: Does this cell line respond to clinically relevant compounds?
Yes. The assay has been validated with native GIP peptides, GIP analogs, and dual GLP-1/GIP agonists, ensuring physiologically relevant and translational results.
Q4: Is any cell line engineering required?
No. This is a fully validated, ready-to-use stable cell line—simply thaw, culture, treat, and read.
Q5: What applications is this cell line suitable for?
GPCR activation assays Ligand screening and potency ranking Functional characterization of GIP analogs High‑throughput screening (HTS) for GIPR modulators Pathway analysis of cAMP/CREB signaling Validation of GIPR agonists and antagonists.
Q6: How many passages can the cell line be used for?
We recommend use within 20-25 passages from thawing for consistent GPCR and reporter expression.
Q7: Do I need to serum‑starve the cells before stimulation?
2–4 hours of serum starvation improve assay reproducibility by reducing background CREB activity. Some users observe acceptable results with no starvation, but optimization is recommended.
Q8: What QC tests are performed before shipment?
- CREB reporter functional validation
- Mycoplasma negativity testing
- Viability check post‑thaw
- Stability verification under selection antibiotics
