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Applications: Great for screening small molecular inhibitors for drug discovery and HTS applications.
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 PCSK9binding to LDLR in a homogeneous 384 reaction format. This FRET-based assay requires no time-consuming washingsteps, making it especially suitable for high throughput screening applications. Theassay procedure is straightforward and simple; a sample containing europium-labeled(Eu) LDLR ectodomain, dye-labeled acceptor, biotin-labeled PCSK9, and an inhibitor isincubated for two hours. Then, the fluorescence intensity is measured using afluorescence reader.
Storage Stability: At least 6 months from date of receipt when stored as directed.
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.
Uniprot: Q8NBP7
Warnings: Avoid freeze/thaw cycles.
Biosafety Level: Not applicable (BSL-1)
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