PCSK9

Proprotein convertase subtilisin/kexin type 9

The protein convertase subtilisin/kexin type 9 (PCSK9) is an enzyme encoded by the PCSK9 gene located on human chromosome 1. It is the ninth member of the protein convertase family, a group of enzymes that can activate homologous genes found in many species^[1]. PCSK9 is a liver-synthesized protease that plays a major role in regulating the levels of low-density lipoprotein receptors (LDLR) on the surface of liver cells and can inhibit the LDLR recycling pathway. PCSK9 binds to LDLR on the surface of liver cells, escorts LDLR to lysosomes for degradation, and prevents LDLR from recirculating to the cell membrane, effectively increasing the level of circulating LDL. Therefore, inhibiting the activity of the PCSK9 protease can down-regulate circulating LDL levels. PCSK9 is closely associated with various cardiovascular diseases, especially hypercholesterolemia and atherosclerosis^[2].

References:

[1]. Horton JD, et al. PCSK9: a convertase that coordinates LDL catabolism. J Lipid Res. 2009 Apr;50 Suppl(Suppl):S172-7. [Content Brief]

[2]. Peterson AS, et al. PCSK9 function and physiology. J Lipid Res. 2008 Jun;49(6):1152-6. [Content Brief]

PCSK9 Related Products (95):

By Effects:	Inhibitors (81) Degraders (3) Modulators (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-RS10177

PCSK9 Human Pre-designed siRNA Set A	Inhibitor
PCSK9 Human Pre-designed siRNA Set A contains three designed siRNAs for PCSK9 gene (Human), as well as a negative control, a positive control, and a FAM-labeled negative control.

HY-148689A

SPC4061 sodium	Inhibitor
SPC4061 an antisense nucleotide, sodium is a potent PCSK9 inhibitor. SPC4061 targets the lock-in nucleic acid (LNA) of PCSK9 for the study of hypercholesterolemia and related diseases.

HY-134482

PCSK9-IN-1	Inhibitor
PCSK9-IN-1 is a novel and highly potent cyclic peptide PCSK9 inhibitor with a K_i value of 1.46 nM.

HY-158825

Cepadacursen sodium
Cepadacursen sodium is a liver-targeting antisense oligonucleotide (ASO), inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9) protein synthesis. Cepadacursen sodium can be used for hypercholesterolemia research and the prevention of atherosclerotic cardiovascular disease (ASCVD).

HY-12090R

Anacetrapib (Standard)	Inhibitor
Anacetrapib (Standard) is the analytical standard of Anacetrapib. This product is intended for research and analytical applications. Anacetrapib is a potent CETP inhibitor, with IC50s of 7.9±2.5 nM and 11.8±1.9 nM for rhCETP and C13S CETP mutant, respectively.

HY-175189

PCSK9-IN-33	Inhibitor
PCSK9-IN-33 (Compound 1'f) is a PCSK9 inhibitor with an IC₅₀ of 161 nM. PCSK9-IN-33 can be used for hypercholesterolemia research.

HY-164344

PCSK9 allosteric binder-1
PCSK9 allosteric binder-1 (example 70) is a PCSK9 allosteric binder. PCSK9 allosteric binder-1 can be used in the study of cardiovascular diseases.

HY-155415

PCSK9-IN-20	Inhibitor
PCSK9-IN-20 (Compound 3i) is a PCSK9 inhibitor with an IC₅₀ of 3.96 µM. PCSK9-IN-20 decreases PCSK9 and increases LDLR protein expression in vitro.

HY-101832R

SBC-110736 (Standard)	Inhibitor
SBC-110736 (Standard) is the analytical standard of SBC-110736 (HY-101832). This product is intended for research and analytical applications. SBC-110736 is a proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitor extracted from patent WO2014150395A1.

HY-168156

PCSK9-IN-32	Inhibitor
PCSK9-IN-32 (compund 8) is a PCSK9[1:33]-GFP translation inhibitor.

HY-158827B

AZD8233 sodium scrambled negative control
AZD8233 sodium scrambled negative control is the sequence scrambled negative control of AZD8233 sodium.

HY-161938

BRD8518	Inhibitor
BRD8518 is a PCSK9 inhibitor (EC₅₀=0.23 μM). BRD8518 lowers blood lipids by upregulating LDLR expression and stimulating LDL uptake. BRD8518 can be used in the study of cardiovascular diseases.

HY-158827

AZD8233
AZD8233, a liver-targeting antisense oligonucleotide (ASO), inhibits proprotein convertase subtilisin/kexin type 9 (PCSK9) protein synthesis. AZD8233 increases the available LDL receptors by reducing PCSK9 levels, thereby clearing LDL from the blood and decreasing LDL-C levels.

HY-149310A

Dim16 hydrochloride	Inhibitor
Dim16 hydrochloride is a dual PCSK9 inhibitor and HMG-CoAR inhibitor, with an IC₅₀ of 0.8 nM against human PCSK9 and an IC₅₀ of 146.8 μM against HMG-CoAR. Dim16 hydrochloride disrupts the PCSK9-LDLR protein-protein interaction, inhibits the catalytic activity of HMG-CoAR, enhances cellular uptake of extracellular LDL, and suppresses PCSK9-induced platelet aggregation. Dim16 hydrochloride can be used in research related to hypercholesterolemia.

HY-158825A

Cepadacursen sodium scrambled negative control
Cepadacursen sodium scrambled negative control is the sequence scrambled negative control of Cepadacursen sodium.

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