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 (84):

By Effects:	Inhibitors (73) Degraders (3) Modulators (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-161434

PCSK9-IN-26	Inhibitor
PCSK9-IN-26 (Compound 116) is an PCSK9 inhibitor (IC₅₀ < 1 nM). PCSK9-IN-26 can be used for metabolic research.

HY-161942

PCSK9-IN-31	Inhibitor
PCSK9-IN-31 (Compound WX002) is an orally active PCSK9 inhibitor. PCSK9-IN-31 can lower low-density lipoprotein cholesterol (LDL-C) and total cholesterol (TC) in high cholesterol fed model rats.

HY-176043

PCSK9 autophagic degrader 2	Degrader
PCSK9 autophagic degrader 2 (W6) is a PCSK9 targeted autophagosome, with an DC₅₀ of 20.6 nM. PCSK9 autophagic degrader 2 (W6) demonstrates comparable antiatherosclerosis effect and exhibits a K_D of 2.5 μM for LC3B (Pink: PCSK9 ligand HY-176044; Blue: LC3B ligand HY-176045; Black: linker HY-141373).

HY-153391

PCSK9-IN-14	Inhibitor
PCSK9-IN-14 (compound Ia-8) is a potent PCSK9 inhibitor.

HY-161435

PCSK9-IN-27	Inhibitor
PCSK9-IN-27 (Compound 108) is a PCSK9 inhibitor (IC₅₀: 3.4 nM). PCSK9-IN-27 reduces LDLR degradation and increases LDL-C uptake.

HY-153453

PCSK9-IN-17	Inhibitor
PCSK9-IN-17 is a PCSK9 inhibitor. PCSK9-IN-17 can be used for the research of cholesterol metabolism (WO2020150474A1, compound 105).

HY-163141

PCSK9-IN-24	Inhibitor
PCSK9-IN-24 (Compound OY3) is a compound that targets PCSK9. PCSK9-IN-24 reduces PCSK9 levels and increases LDL uptake and may be used in atherosclerosis research.

HY-N10702

PCSK9-IN-9	Inhibitor
PCSK9-IN-9 is an isocoumarins of natural origin. PCSK9-IN-9 can inhibit proprotein convertase subtilisin-kexin type 9 (PCSK9), IDOL, and SREBP2 mRNA expression. PCSK9-IN-9 inhibits PCSK9 with an IC₅₀ value of 11.9 μM.

HY-146085

PCSK9 modulator-4	Modulator
PCSK9 modulator-4 (Compound 21) is a potent modulator of PCSK9 with an EC₅₀ value of 0.15 nM. PCSK9 is a recently validated target for lowering low-density lipoprotein cholesterol (LDL-C). PCSK9 modulator-4 has the potential for the research of hyperlipidemia.

HY-153451

PCSK9-IN-15	Inhibitor
PCSK9-IN-15 (compound 5) is a potent inhibitor of proprotein convertase subtilisin/kexin 9 (PCSK9, K_D <200 nM). PCSK9 is involved in cholesterol metabolism and regulates levels of low-density lipoprotein cholesterol (LDL-C) in the blood. PCSK9- in -15 can be used to study cholesterol-lowering and dyslipidemia.

HY-161941

MeIm	Inhibitor
MeIm (compound 7) is a high-affinity PCSK9 targeting peptide mimetic with cholesterol-lowering activity. MeIm increases cellular uptake of LDL (EC₅₀=6.04 μM) by inhibiting the binding of PCSK9 to LDLR (IC₅₀=11.2 μM). MeIm can be used in the study of cardiovascular diseases.

HY-132897

PCSK9-IN-2	Inhibitor
PCSK9-IN-2 is a novel small molecule inhibitor of PCSK9-LDLR protein–protein interaction (PPI) with an IC₅₀ value of 7.57 μM.

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 treatment 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-159595

PCSK9-IN-29	Inhibitor	99.44%
PCSK9-IN-29 is a lipid-lowering agent. PCSK9-IN-29 can increase low-density lipoprotein receptor (LDLR) protein expression and decrease PCSK9 protein expression in hepG2 cells. PCSK9-IN-29 can reduce the levels of serum LDL-C, TC, and liver enzyme ALT in crab eating macaques fed a high-fat diet, lower body weight and fat, and increase bone mineral content. PCSK9-IN-29 can be used for research on non-alcoholic fatty liver disease and obesity.

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.

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