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 scree
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
UniProt Q8NBP7
Synonym(s): pcsk9, cholesterol, LDL, kexin
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.
Instructions for use: See assay kit data sheet for detailed protocol.
Storage / Stability: At least 6 months from date of receipt when stored as directed.
Application(s): Great for screening small molecular inhibitors for drug discovery and HTS applications.
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
Warning(s): Avoid freeze/thaw cycles.
Scientific Category: PCSK9-LDLR TR-FRET Assay Kit
Product Type: