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 (83):

By Effects:	Inhibitors (72) Degraders (3) Modulators (3)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-P99187

Bococizumab	Inhibitor	99.80%
Bococizumab (PF-04950615) is an anti-human PCSK9 inhibitory antibody that reduces LDL cholesterol levels. Bococizumab can be used in the research of hypercholesterolemia.

HY-132591A

Inclisiran sodium	Inhibitor	98.10%
Inclisiran sodium is a double-stranded small interfering RNA (siRNA) molecule. Inclisiran sodium inhibits the transcription of PCSK9. Inclisiran sodium inhibits Pyroptosis, activates PPARγ, and reduces NLRP3, cleaved caspase-1, IL-1β, and IL-18. Inclisiran sodium has anti-inflammatory, lipid-regulating and anti-atherosclerotic activities. Inclisiran sodium can be used in researches of hyperlipidemia and cardiovascular disease (CVD).

HY-120088A

PF-06446846 hydrochloride	Inhibitor	99.44%
PF-06446846 hydrochloride is an orally active and highly selective inhibitor of translation of Proprotein convertase subtilisin/kexin type 9 (PCSK9). PF-06446846 hydrochloride inhibits PCSK9 by inducing the ribosome to stall around codon 34.

HY-148673

AZD0780	Inhibitor	99.97%
AZD0780 (PCSK9-IN-12) is an orall active PCSK9 inhibitor. PCSK9-IN-12 has bind affinity for PCSK9 with a K_d value of <200 nM. AZD0780 binds to a pocket in the PCSK9 C-terminal domain and does not affect the PCSK9-LDL receptor (LDLR) interaction. AZD0780 inhibits lysosomal trafficking of PSCK9-LDLR complexes and prevents PCSK9-induced LDLR degradation. PCSK9-IN-12 can be used for the research of hypercholesterolemia.

HY-P9928

Alirocumab	Inhibitor
Alirocumab is an anti-PCSK9 human monoclonal antibody. Alirocumab inhibits PCSK9. Alirocumab reduces NLRP3 inflammasome, regulates Nrf2/HO-1, HMGB1/NF-κB and Fractalkine/CX3CR1. Alirocumab increases the ability of the liver to bind LDL-cholesterol (LDL-C) and reduces levels of LDL-C in blood. Alirocumab improves atherosclerosis and inflammation.

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-P991343

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

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-132591

Inclisiran	Inhibitor	99.80%
Inclisiran is a double-stranded small interfering RNA (siRNA) molecule. Inclisiran inhibits the transcription of PCSK9. Inclisiran inhibits Pyroptosis, activates PPARγ, and reduces NLRP3, cleaved caspase-1, IL-1β, and IL-18. Inclisiran has anti-inflammatory, lipid-regulating and anti-atherosclerotic activities. Inclisiran can be used in researches of hyperlipidemia and cardiovascular disease (CVD).

HY-12402

SBC-115076	Inhibitor	99.28%
SBC-115076 is a potent proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. PCSK9 is a proprotein convertase, which plays a crucial role in LDL receptor metabolism.

HY-P2276

Pep2-8	Inhibitor	99.74%
Pep2-8 is a PCSK9 inhibitor with a binding K_D of 0.7 μM and an IC₅₀ of 1.4 μM.

HY-P4153

Enlicitide chloride	Inhibitor	99.63%
Enlicitide chloride is an orally active inhibitor for PCSK9 that blocks the interaction between LPL receptor and PSCK9, with an IC₅₀ of 2.5 nM. Enlicitide chloride can be used in the study of cardiovascular diseases such as atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome or related cardiovascular and cardiometabolic disorders.

HY-143221

AS-Inclisiran sodium	Inhibitor
AS-Inclisiran sodium is the antisense of Inclisiran. Inclisiran (ALN-PCSsc) is a double-stranded small interfering RNA (siRNA) molecule that inhibits the transcription of PCSK-9. Inclisiran can be used for hyperlipidemia and cardiovascular disease (CVD) research.

HY-152221

PCSK9-IN-10	Inhibitor	98.89%
PCSK9-IN-10 is a potent and orally active PCSK9 inhibitor with an IC₅₀ value of 6.4 µM. PCSK9-IN-10 increases the expression of LDLR protein and decreases the expression of PCSK9. PCSK9-IN-10 reduces atherosclerosis progression. PCSK9-IN-10 has the potential for the research of hyperlipidemia.

HY-P9928A

Alirocumab (anti-PCSK9)	Inhibitor	98.24%
Alirocumab (anti-PCSK9) is an anti-PCSK9 human monoclonal antibody. Alirocumab (anti-PCSK9) inhibits PCSK9. Alirocumab (anti-PCSK9) reduces NLRP3 inflammasome, regulates Nrf2/HO-1, HMGB1/NF-κB and Fractalkine/CX3CR1. Alirocumab (anti-PCSK9) increases the ability of the liver to bind LDL-cholesterol (LDL-C) and reduces levels of LDL-C in blood. Alirocumab (anti-PCSK9) improves atherosclerosis and inflammation.

HY-143219

SS-Inclisiran sodium	Inhibitor	98.88%
SS-Inclisiran (sodium) is a sense strand of Inclisiran. Inclisiran is a double-stranded small interfering RNA (siRNA) molecule that inhibits the transcription of PCSK-9.

HY-12090

Anacetrapib	Inhibitor	99.25%
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-152223

PCSK9-IN-11	Inhibitor	99.30%
PCSK9-IN-11 (compound 5r) is a potent and orally active PCSK9 inhibitor. PCSK9-IN-11 exhibits PCSK9 transcriptional inhibitory activity in HepG2 cells, with an IC₅₀ of 5.7 μM. PCSK9-IN-11 increases LDL receptor (LDLR) protein level. PCSK9-IN-11 can be used for atherosclerosis research.

HY-101354

R-IMPP	Inhibitor	98.76%
R-IMPP (PF-00932239) is an anti-secretagogue of PCSK9 (IC₅₀=4.8 μM), which targets the 80S ribosome to inhibit PCSK9 protein translation.

HY-W510159

5-O-Methylembelin	Inhibitor	98.84%
5-O-Methylembelin is a natural isocoumarin that inhibits PCSK9, inducible degrader of the low-density lipoprotein receptor (IDLR), and sterol regulatory element binding protein 2 (SREBP2) mRNA expression.

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