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-101832
    SBC-110736
    		Inhibitor 99.93%
    SBC-110736 is a proprotein convertase subtilisin kexin type 9 (PCSK9) inhibitor extracted from patent WO2014150395A1.
    SBC-110736
  • HY-130245
    PCSK9 degrader 1
    		Degrader 98.33%
    PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor.
    PCSK9 degrader 1
  • HY-141714
    SBC-115337
    		Inhibitor 98.02%
    SBC-115337, as a potent benzofuran compound, is a PCSK9 inhibitor with an IC50 value of 0.5 μM.
    SBC-115337
  • HY-148758
    PCSK9-IN-13
    		Inhibitor 98.00%
    PCSK9-IN-13(compound 3f) is a potent PCSK9 inhibitor, which can antagonize low-density lipoprotein (LDL) receptor binding by binding to PCSK9, with an IC50 of 537 nM.
    PCSK9-IN-13
  • HY-112598A
    PF-06815345 hydrochloride
    		Inhibitor 98.15%
    PF-06815345 hydrochloride is an orally active and potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) with an IC50 value of 13.4 μM. PF-06815345 hydrochloride significantly decreases the PCSK9 level in vivo in mouse.
    PF-06815345 hydrochloride
  • HY-148687
    SPC5001
    		Inhibitor
    SPC5001 is a locked nucleic acid (LNA)-modifed antisense oligonucleotide (ASO) complementary to human PCSK9 (proprotein convertase subtilisin/kexin type 9) mRNA. SPC5001 can be used for the research of hypercholesterolemia. SPC5001 sequence: 5′-TGmCTACAAAACmCmCA-3′.
    SPC5001
  • HY-P2276A
    Pep2-8 TFA
    		Inhibitor 99.44%
    Pep2-8 is a peptide which has enhanced the antagonistic activity of proprotein convertase subtilin/ kexin 9 type (PCSK9).
    Pep2-8 TFA
  • HY-161940
    PCSK9-IN-30
    		Inhibitor
    PCSK9-IN-30 (Compound 3f) is a PCSK9 inhibitor. PCSK9-IN-30 interacts with a cryptic binding groove of PCSK9, inhibiting the binding of PCSK9 to the low-density lipoprotein receptor (LDLR) (IC50 = 537 nM), restoring the uptake of low-density lipoprotein (LDL) by liver cells, and ultimately reducing plasma cholesterol levels. PCSK9-IN-30 exhibits good bioavailability in mice and can be used for research in the field of cardiovascular diseases.
    PCSK9-IN-30
  • HY-P99822
    Recaticimab
    		Inhibitor 99.71%
    Recaticimab (SHR-1209) is an orally active humanized monoclonal antibody targeting PCSK9. Recaticimab binds PCSK9 with high affinity, increases the level of low density lipoprotein receptor on the surface of liver cells, and decreases the level of low density lipoprotein cholesterol in plasma. Recaticimab can be used in the study of hypercholesterolemia and hyperlipidemia.
    Recaticimab
  • HY-112598
    PF-06815345
    		Inhibitor
    PF-06815345 is an orally active and potent inhibitor of proprotein convertase subtilisin/kexin type 9 (PCSK9) with an IC50 value of 13.4 μM. PF-06815345 significantly decreases the PCSK9 level in vivo in mouse.
    PF-06815345
  • HY-163794
    DC371739
    		Inhibitor
    DC371739 is a potent and orally activity PCSK9 inhibitor. DC371739 decreases the mRNA expression of PCSK9 and ANGPTL3. DC371739 decreases the protein expression of PCSK9 and increases the protein expression of LDLR. DC371739 has the potential for the research of hyperlipidemia.
    DC371739
  • HY-157434
    PCSK9-IN-23
    		Inhibitor 99.57%
    PCSK9-IN-23 (compound 5C) is a potent PCSK9 inhibitor. PCSK9-IN-23 blocks PCSK9 secretion from HepG2 cells, significantly increases LDL receptor (LDLR) expression.
    PCSK9-IN-23
  • 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).
    Cepadacursen sodium
  • HY-139998
    PCSK9-IN-3
    		Inhibitor
    PCSK9-IN-3 is a novel, highly potent, and orally bioavailable next-generation tricyclic peptide PCSK9 inhibitor.
    PCSK9-IN-3
  • HY-120088
    PF-06446846
    		Inhibitor
    PF-06446846 is an orally active proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. PF-06446846 directly and selectively inhibits translation of PCSK9 by stalling the 80S ribosome in the proximity of codon region.
    PF-06446846
  • HY-P99871
    Ebronucimab
    		Inhibitor
    Ebronucimab (AK102) is an IgG1-λ2 antibody targeting PCSK9 and is primarily expressed by CHO DG44 (Chinese Hamster Ovary) cells.
    Ebronucimab
  • HY-P99626
    Frovocimab
    		Inhibitor
    Frovocimab (LY 3015014) is a humanized IgG4 monoclonal antibody (mAb) that neutralizes PCSK9. Frovocimab inhibits PCSK9 binding to LDL receptor (LDLR) while permitting the normal proteolytic cleavage of the bound intact PCSK9.
    Frovocimab
  • HY-P99773
    Ongericimab
    		Inhibitor
    Ongericimab (JS002) is a humanized anti-PCSK9 monoclonal antibody. Ongericimab has lipid-lowering efficacy. Ongericimab can be used in research of hypercholesteremia and hyperlipidemia.
    Ongericimab
  • 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.
    Lerodalcibep
  • HY-148626
    CVI-LM001
    		Inhibitor
    CVI-LM001 is an inhibitor PCSK 9. CVI-LM001 inhibits the interaction of PCSK9 with low-density lipoprotein receptor (LDLR), regulates the level of low-density lipoprotein cholesterol (LDL-C) in the blood, and exhibits lipid-lowering efficacy.
    CVI-LM001