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
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.
Great for screening small molecular inhibitors for drug discovery and HTS applications.
At least 6 months from date of receipt when stored as directed.
LDLR-Eu: 2 µg; -80°C PCSK9, Biotinylated: 30 µg; -80°C Dye-labeled acceptor: 2 x 10 µl; -20°C 3x PCSK9 TR-FRET Assay Buffer: 4 ml; -20°C White, Nonbinding, low volume, 384-well microtiter plate: 1; Room temp.