| 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 |
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| 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. |
| Format: | |
| 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: | |