PCSK9(D374T), Biotin-labeled

Description: Human proprotein convertase subtilisin/kexin type 9 (PCSK9), also known as FH3, HCHOLA3, and PC9, GenBank Accession No. NM_174936, a.a. 31- 692(end), with C-terminal His- and Avi-tags and a D374T mutation, MW=73.8 kDa, expressed in an HEK293 cell ex
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. The D374T mutation results in higher affinity of PCSK9 for LDLR.
UniProt Q8NBP7
Synonym(s): Proprotein convertase subtilisin/kexin type 9, FH3, HCHOLA3, PC9
Assay Conditions: Reaction was performed using PCSK9(D374T)-LDLR TR-FRET Assay Kit (Cat. #72011). Briefly, 5 ng of europium-labeled LDLR were mixed with varying amounts of PCSK9(D374T) and dyelabeled acceptor in PCSK9 TR-FRET assay buffer and incubated at RT for 2 hr. Donor emission was read at 620 nm followed by acceptor emission at 665 nm.
Formulation: 40 mM Tris-HCl pH 8.0, 110 mM NaCl, 2.2 mM KCl, and 20% glycerol
Format: Aqueous buffer solution
Storage / Stability: >6 months at
Application(s): Useful for the study of enzyme kinetics, binding studies, screening inhibitors, and selectivity profiling.
Reference(s): 1. Chan, J.C. et al. (2009). Proc. Natl. Acad. Sci. USA, 106: 9820-9825. 2. Liang, H., et al. (2012). J. Pharmacol. Exp. Ther. 340: 2289-236.
Warning(s): Avoid freeze/thaw cycles. Storing diluted enzyme is not recommended, if necessary, use carrier protein (BSA 0.1
Scientific Category: PCSK9(D374T), Biotin-labeled
Product Type: