VEGFR1:VEGF165 (Biotinylated) Inhibitor Screening Chemiluminescence Assay Kit

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Application: Screen or titrate small molecule inhibitors or antibodies that block VEGFR1 binding to VEGF165 for drug discovery and high-throughput screening (HTS) applications.

Background: VEGF165 (Vascular Endothelial Growth Factor 165), a potent isoform of VEGF-A, belongs to the VEGF family of homodimer glycoproteins and is produced and secreted by various cells when angiogenesis is required. Angiogenesis involves endothelial cell proliferation, migration, and formation of blood vessels, which under normal conditions serve to provide nutrients and oxygen to tissues during development or wound healing. However, tumor cells can promote new blood vessel formation by secreting pro-angiogenesis factors. VEGF-A can bind to both VEGFR1 (Vascular Endothelial Growth Factor Receptor 1) and VEGFR2, also known as KDR (kinase insert domain receptor), on the surface of endothelial cells or cancer cells. VEGFR2 is considered the main signaling receptor, while VEGFR1 leads to a weak signaling and can be seen as a decoy receptor. Ligand binding induces VEGFR2 receptor dimerization and activates its tyrosine kinase activity.  As a result, multiple downstream signaling cascades, including the MAPK (mitogen activated protein kinase) pathway, get activated.  The VEGF-VEGFR signal pathway has been a significant target in therapeutic strategies aimed at controlling angiogenesis in diseases like cancer and AMD (age macular degeneration), and several small molecules, neutralizing antibodies and blockers have been FDA-approved. However, the development of drug resistance is still a challenge. The use of combinatory therapy or development of new generation drugs will continue to benefit cancer therapy.

Contraindications: The DMSO concentration in the final reaction should be ‰¤1%.

Description: The VEGFR1:VEGF165 [Biotinylated] Inhibitor Screening Chemiluminescence Assay Kit is an ELISA designed for screening and profiling molecules that block the binding between VEGFR1 (vascular endothelial growth factor receptor 1, also known as fms related receptor tyrosine kinase 1) and VEGF165 (vascular endothelial growth factor 165). This kit comes in a convenient 96-well format, with enough recombinant biotin-labeled VEGF165 (amino acids 27-191(end)), purified VEGFR1 (amino acids 27-756), streptavidin-labeled HRP, and assay buffer for 100 binding reactions.A 96-well plate is coated with VEGFR1 protein. After blocking, the plate is pre-incubated with an inhibitor or neutralizing antibody. After incubation with Biotin-VEGF165, the plate is washed and Streptavidin-HRP is added. The ELISA ECL substrate is added, and the resulting signal can be measured using a chemiluminescence microplate reader. The chemiluminescence signal is proportional to the binding of VEGFR1 to VEGF165.

Storage Stability: This assay kit will perform optimally for up to 6 months from date of receipt when the materials are stored as directed.

Warnings: Avoid freeze/thaw cycles

Biosafety Level: Not applicable (BSL-1)

References: Wang L., et al., 2024 Front Pharmacol. 14:1307860.

• Artikelnummer: BPS82632
• Hersteller: BPS Bioscience
• Hersteller Artikelnummer: 82632
• Verpackungseinheit: 96 reactions
• Mengeneinheit: PAK