PCSK9-LDLR TR-FRET Assay Kit

DESCRIPTION

The PCSK9/LDLR TR-FRET Assay Kit is designed to measure the inhibition of PCSK9 binding to LDLR in a homogeneous 384 reaction format. This FRET-based assay requires no time-consuming washing steps, making it especially suitable for high throughput screening applications. The assay procedure is straightforward and simple; a sample containing europium-labeled (Eu) LDLR ectodomain, dye-labeled acceptor, biotin-labeled PCSK9, and an inhibitor is incubated for two hours. Then, the fluorescence intensity is measured using a fluorescence reader.

DETAILS

Notes: MATERIALS OR INSTRUMENTS REQUIRED BUT NOT SUPPLIED: Fluorescent microplate reader capable of measuring Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET) Adjustable micropipettor and sterile tips
Uniprot: Q8NBP7
Shiptemp: -80°C (dry ice)
Synonyms: pcsk9, cholesterol, LDL, kexin
Warnings: Avoid freeze/thaw cycles.
Category: Cholesterol-Related/Assay Kit
Background: PCSK9 is a crucial player in the regulation of plasma cholesterol homeostasis. It binds to the ectodomain of hepatic low-density lipid receptor family members: low density lipoprotein receptor (LDLR), very low density lipoprotein receptor (VLDLR), apolipoprotein E receptor (LRP1/APOER) and apolipoprotein receptor 2 (LRP8/APOER2), and promotes their degradation. PCSK9 acts via a non-proteolytic mechanism to enhance the degradation of the hepatic LDLR through a clathrin LDLRAP1/ARH-mediated pathway. May prevent the recycling of LDLR from endosomes to the cell surface or direct it to lysosomes for degradation
Description: The PCSK9/LDLR TR-FRET Assay Kit is designed to measure the inhibition of PCSK9 binding to LDLR in a homogeneous 384 reaction format. This FRET-based assay requires no time-consuming washing steps, making it especially suitable for high throughput screening applications. The assay procedure is straightforward and simple; a sample containing europium-labeled (Eu) LDLR ectodomain, dye-labeled acceptor, biotin-labeled PCSK9, and an inhibitor is incubated for two hours. Then, the fluorescence intensity is measured using a fluorescence reader.
Methodology: TR-FRET
Supplied As: Kit comes in a convenient format with purified ATAD2A, ligands, Tb donor, dye-labeled acceptor, assay buffer and microtiter plate to perform 384 reactions.
Unspsc Code: 41121811
Unspsc Name: Laboratory microchemistry kits
Applications: Great for screening small molecular inhibitors for drug discovery and HTS applications.
Product Type: Assay Kit
Biosafety Level: Not applicable (BSL-1)
Related Products: 72002, 72011, 71204, 79079
Storage Stability: At least 6 months from date of receipt when stored as directed.
Scientific Category: Cholesterol-Related
Instructions for Use: See assay kit datasheet for detailed protocol.