2. Signaling Pathways
  3. Metabolic Enzyme/Protease
  4. PCSK9

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].

PCSK9 Related Products (79):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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.
    PCSK9-IN-9
  • 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.
    PCSK9 modulator-4
  • HY-153451
    PCSK9-IN-15
    		Inhibitor
    PCSK9-IN-15 (compound 5) is a potent inhibitor of proprotein convertase subtilisin/kexin 9 (PCSK9, KD <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.
    PCSK9-IN-15
  • 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.
    MeIm
  • 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.
    PCSK9-IN-2
  • 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.
    PCSK9 Human Pre-designed siRNA Set A
    PCSK9 Human Pre-designed siRNA Set A
  • HY-161939
    7030B-C5
    		Inhibitor
    7030B-C5 is a PCSK9 inhibitor (IC50=1.61 μM). 7030B-C5 can significantly reduce plasma cholesterol and triglyceride (TG) levels in vivo and slow the progression of atherosclerosis. 7030B-C5 can be used in the study of cardiovascular diseases.
    7030B-C5
  • 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.
    SPC4061 sodium
  • HY-134482
    PCSK9-IN-1
    		Inhibitor
    PCSK9-IN-1 is a novel and highly potent cyclic peptide PCSK9 inhibitor with a Ki value of 1.46 nM.
    PCSK9-IN-1
  • HY-162562
    E28362
    		Inhibitor
    E28362 is a novel small molecule PCSK9 inhibitor. E28362 blocks the interaction between PCSK9 and LDLR, thereby preventing the degradation of LDLR and maintaining cholesterol homeostasia. E28362 is a promising lead compound for the study of hyperlipidemia and atherosclerosis.
    E28362
  • HY-159595
    PCSK9-IN-29
    		Inhibitor
    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.
    PCSK9-IN-29
  • 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.
    PCSK9 allosteric binder-1
  • HY-P99251
    Lodelcizumab
    		Inhibitor
    Lodelcizumab is a monoclonal antibody targeting PCSK9. Lodelcizumab can be used for the research of hypercholesterolemia.
    Lodelcizumab
  • 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.
    PCSK9-IN-20
  • HY-168156
    PCSK9-IN-32
    		Inhibitor
    PCSK9-IN-32 (compund 8) is a PCSK9[1:33]-GFP translation inhibitor.
    PCSK9-IN-32
  • 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.
    BRD8518
  • HY-158827A
    AZD8233 sodium
    AZD8233 sodium, a liver-targeting antisense oligonucleotide (ASO), inhibits subtilisin/kexin type 9 (PCSK9) protein synthesis. AZD8233 sodium increases the available LDL receptors by reducing PCSK9 levels, thereby clearing LDL from the blood and decreasing LDL-C levels.
    AZD8233 sodium
  • HY-N13083
    PCSK9-IN-28
    		Inhibitor
    PCSK9-IN-28 (Compound C11) is a PCSK9 inhibitor that can be isolated from Euphorbia esula. By binding to HNF1α, PCSK9-IN-28 inhibits PCSK9 transcription by binding to HNF1α and affecting its nuclear distribution, thereby enhancing LDLR and promoting LDL uptake. PCSK9-IN-28 exhibits significant lipid-lowering activity in the high-fat diet (HFD) mouse model and can be used in the study of hyperlipidemia.
    PCSK9-IN-28
  • 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.
    AZD8233