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 (95):

Cat. No. Product Name Effect Purity Chemical Structure
  • 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.
    PCSK9-IN-11
  • HY-101354
    R-IMPP
    		Inhibitor 99.93%
    R-IMPP (PF-00932239) is an anti-secretagogue of PCSK9 (IC50=4.8 μM), which targets the 80S ribosome to inhibit PCSK9 protein translation.
    R-IMPP
  • 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-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-101832
    SBC-110736
    		Inhibitor 99.55%
    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-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-P2276A
    Pep2-8 TFA
    		Inhibitor 98.78%
    Pep2-8 is a peptide which has enhanced the antagonistic activity of proprotein convertase subtilin/ kexin 9 type (PCSK9).
    Pep2-8 TFA
  • 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-120088
    PF-06446846
    		Inhibitor 98.35%
    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-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-P99822
    Recaticimab
    		Inhibitor 99.71%
    Recaticimab (SHR-1209) is a humanized IgG1 mAb that selectively targets PCSK9. Recaticimab reduces low-density lipoprotein cholesterol (LDL-C), non-high-density lipoprotein cholesterol (non-HDL-C), apolipoprotein B (ApoB), triglyceride (TG), and lipoprotein(a) levels. Recaticimab can be used for hyperlipidemia research.
    Recaticimab
  • HY-P99816
    Ralpancizumab
    		Inhibitor
    Ralpancizumab is a selective PCSK9 inhibitor with potential application in hemorrhagic stroke.
    Ralpancizumab
  • HY-161939
    7030B-C5
    		Inhibitor 99.78%
    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-P99251
    Lodelcizumab
    		Inhibitor ≥99.0%
    Lodelcizumab is a monoclonal antibody targeting PCSK9. Lodelcizumab can be used for the research of hypercholesterolemia.
    Lodelcizumab
  • 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-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-162562
    E28362
    		Inhibitor
    E28362 is an orally active lipid-lowering agent and a selective PCSK9 antagonist. E28362 blocks the interaction between PCSK9 and LDLR, and induces PCSK9 degradation via the ubiquitin-proteasome pathway. E28362 significantly increases the levels of cell surface and total LDLR proteins, enhances low-density lipoprotein uptake, thereby effectively reducing plasma lipids, hepatic cholesterol and triglyceride levels. E28362 shows no obvious cytotoxicity at high concentrations, and significantly attenuates atherosclerotic lesions in animal models. E28362 is an important molecule in research of hyperlipidemia and atherosclerosis.
    E28362