PCSK9(D374T)-LDLR TR-FRET Assay Kit

Catalog #

72011

$765 *

Size: 384 reactions

Qty

Bulk/Custom

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*US Pricing only. For international pricing, please contact your local distributor.

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Description

The PCSK9(D374T)-LDLR TR-FRET Assay Kit is designed to measure the inhibition of the high affinity PCSK9 mutant (D374T) binding to LDLR in a homogeneous 384 reaction format. The PCSK9 Assay Kit 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(D374T), and an inhibitor is incubated for two hours. Then, the fluorescence intensity is measured using a fluorescence reader. The kit contains enough purified proteins, Eu-donor, dye-labeled acceptor and assay buffer to perform 384 reactions.

Need us to run inhibitor screens or profile your compounds against PCSK9(D374T)-LDLR? Check out our PCSK9 Screening Services.

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Synonyms

pcsk9, cholesterol, LDL, kexin, PCSK9 Assay Kit

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Product Data Gallery

Product Info

Storage and Usage

Citations

Assay Kit Format

TR-FRET

Format

Catalog #	Component	Amount	Storage
79079	LDLR-Eu*	2 µg	-80°C	*Avoid freeze/ thaw cycles*
71211	PCSK9(D374T), Biotinylated*	25 µg	-80°C
	Dye-labeled acceptor	2 x 10 µl	-20°C
33298	3x PL-01 Assay Buffer	4 ml	-20°C
79969	White, Nonbinding, low volume, 384-well microtiter plate	1	Room Temp

*The concentration of LDLR-Eu and PCSK9 are lot-specific and will be indicated on the tubes containing the protein

UniProt #

Q8NBP7

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.

References

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.

Storage/Stability

At least 6 months from date of receipt when stored as directed.

Instructions for Use

See assay kit data sheet for detailed protocol.

Applications

Useful for screening small molecular inhibitors for drug discovery and HTS applications.

Shipping Temperature

-80°C

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

Disclaimers and Limitations

BPS Bioscience assay kits are validated using the listed components according to our specific protocol. Any deviations to kit components or protocols, such as using different proteins, cell/tissue lysates, or buffers (including using the same component from other commercial sources) will void any warranties on the performance of the assay kit and is not recommended.

End-users should immediately report any issues to [email protected] upon receipt of the kit, such as missing components, damaged vials, no dry ice, etc.

Scientific Category

Cholesterol Related

Regulatory Status

Research Use Only

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PCSK9(D374T)-LDLR TR-FRET Assay Kit

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