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-P11216

Pep2-8 analogue 18	Inhibitor
Pep2-8 analogue 18 is a high affinity PCSK9 (K_D = 6 nM) inhibitory peptide. Pep2-8 analogue 18 restores LDL uptake in HepG2 cells (EC₅₀ = 175 nM). Pep2-8 analogue 18 has good cellular safety. Pep2-8 analogue 18 can be used for research on cardiovascular conditions.

HY-149310

Dim16	Inhibitor
Dim16 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 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 can be used in research related to hypercholesterolemia.

HY-153454

PCSK9-IN-18	Inhibitor
PCSK9-IN-18 (compound 188) is a potent PCSK9 inhibitor with a K_D value of <200 nM.

HY-147252C

Bezeparsen sodium scrambled negative control	Inhibitor
Bezeparsen sodium scrambled negative control is the sequence scrambled negative control of Bezeparsen sodium.

HY-160036

PCSK9-IN-22	Inhibitor
PCSK9-IN-22 (compound 29) is an orally active inhibitor of PCSK9. PCSK9-IN-22 inhibits the interaction of the protein with LDLR in vivo.

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-132591C

Inclisiran sodium scrambled negative control	Inhibitor
Inclisiran sodium scrambled negative control is the sequence scrambled negative control of Inclisiran sodium.

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-P991343

ALD306	Inhibitor
ALD306 is a human monoclonal antibody (mAb) targeting PCSK9. ALD306 can be used in Hypercholesterolaemia research.

HY-P99696

Lerodalcibep
Lerodalcibep (LIB003) is a recombinant fusion protein of a PCSK9-binding domain (adnectin) and human serum albumin. Lerodalcibep is a Lipid-lowering agent. Lerodalcibep can be used for the research of hypercholesterolemia and cardiovascular diseases.

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-P11071

PCSK9 Inhibitor, EGF-A	Inhibitor
PCSK9 Inhibitor, EGF-A is a PCSK9 inhibitor. PCSK9 Inhibitor, EGF-A is residues 293-334 of the EGF-A domain of the low-density lipoprotein (LDL) receptor. PCSK9 Inhibitor, EGF-A can prevent PCSK9-induced intracellular LDLR degradation. PCSK9 Inhibitor, EGF-A can be used in the study of hypercholesterolemia and premature atherosclerosis.

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.

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