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-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-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-147252A
    Bezeparsen sodium
    		Inhibitor
    Bezeparsen sodium is a PCSK9 synthesis inhibitor.
    Bezeparsen sodium
  • HY-P99552
    Tafolecimab
    		Inhibitor
    Tafolecimab (IBI-306) is a human lgG2 monoclonal antibody that specifically binds PCSK-9 and reduces LDL-C levels by inhibiting PCSK-9-mediated endocytosis of the LDL receptor, which in turn enhances clearance of LDL-C and leads to a reduction in LDL-C levels. Tafolecimab may be used in studies of hypercholesterolaemia.
    Tafolecimab
  • 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-142026
    Vitisin A
    		Inhibitor
    Vitisin A ((+)-Vitisin A) is an orally active natural product with multiple pharmacological activities including anti-inflammatory, anti-tumor, anti-oxidant, anti-pathogenic microorganism, hypoglycemic and lipid-regulating, anti-osteoporotic, neuroprotective and cardiovascular protective effects. Vitisin A exhibits inhibitory effects on human AChE and MAO-B with IC50 values of 1.29 µM and 4.94 µM, respectively. Vitisin A inhibits the ERK, MAPK, NF-κB, STAT1, HMGCR and TRAF6 pathways, downregulates the related phosphorylation and protein expression, while activates the Nrf2/HO-1 pathway and upregulates p21 expression. Vitisin A induces tumor cell apoptosis and cell cycle arrest, inhibits adipogenesis and lipid accumulation, while alleviates oxidative stress, suppresses inflammatory responses, blocks hepatic fibrosis, Cuproptosis and cholesterol synthesis, and increases the expression levels of central BDNF and TrkB. Vitisin A can be used in the research of tumors, infectious diseases, metabolic diseases, bone and joint diseases, liver diseases, skin injuries, as well as neurodegenerative and cognitive dysfunction-related diseases.
    Vitisin A
  • HY-P991721
    Ticalicibart
    		Inhibitor
    Ticalicibart is a humanized IgG4κ monoclonal antibody inhibitor targeting PCSK9. Ticalicibart has anti-hyperlipidaemic activity. Ticalicibart can be used for cardiovascular disease like hypercholesterolaemia research.
    Ticalicibart
  • HY-159595
    PCSK9-IN-29
    		Inhibitor 99.44%
    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-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
  • HY-147252
    Bezeparsen
    		Inhibitor
    Bezeparsen is a PCSK9 synthesis inhibitor.
    Bezeparsen
  • HY-P990485
    Anti-PCSK9 Antibody
    		Inhibitor 98.39%
    Anti-PCSK9 Antibody is a human antibody expressed in CHO, targeting PCSK9. Anti-PCSK9 Antibody contains a huIgG1 heavy chain and a huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for Anti-PCSK9 Antibody can refer to Human IgG1 kappa, Isotype Control (HY-P99001).
    Anti-PCSK9 Antibody
  • HY-128334
    PCSK9 modulator-2
    		Modulator
    PCSK9 modulator-2 (Compound 1) is a potent modulator of PCSK9 with an EC50 value of 202 nM. PCSK9 is a recently validated target for lowering low-density lipoprotein cholesterol (LDL-C). PCSK9 modulator-2 has the potential for the research of hyperlipidemia.
    PCSK9 modulator-2
  • HY-153452
    PCSK9-IN-16
    		Inhibitor
    PCSK9-IN-16 is a potent PCSK9 inhibitor. PCSK9-IN-16 is extracted from patent WO2020150474, example 87, has the potential for hypercholesterolemia and other cardiovascular diseases research.
    PCSK9-IN-16
  • HY-155006
    PCSK9-IN-19
    		Inhibitor
    PCSK9-IN-19 (Compound 1) is a PCSK9 inhibitor. PCSK9-IN-19 can be used for research of high LDL-cholesterol levels and prevention of coronary artery disease.
    PCSK9-IN-19
  • HY-179106
    PCSK9-IN-34
    		Inhibitor
    PCSK9-IN-34 is a small molecule PCSK9 inhibitor. PCSK9-IN-34 can be used for research on cardiovascular conditions.
    PCSK9-IN-34
  • HY-148689
    SPC4061
    		Inhibitor
    SPC4061 an antisense nucleotide, is a potent PCSK9 inhibitor. SPC4061 targets the lock-in nucleic acid (LNA) of PCSK9 for the study of hypercholesterolemia and related diseases.
    SPC4061
  • HY-141724
    PCSK9 ligand 1
    		Inhibitor
    PCSK9 ligand 1 is a selective proprotein convertase substilisin-like/kexin type 9 (PCSK9) ligand. PCSK9 ligand 1 does not affect PCSK9 function.
    PCSK9 ligand 1
  • HY-146084
    PCSK9 modulator-3
    		Modulator
    PCSK9 modulator-3 (Compound 13) is a potent modulator of PCSK9 with an EC50 value of 2.46 nM. PCSK9 is a recently validated target for lowering low-density lipoprotein cholesterol (LDL-C). PCSK9 modulator-3 has the potential for the research of hyperlipidemia.
    PCSK9 modulator-3
  • HY-148689C
    SPC4061 sodium scrambled negative control
    		Inhibitor
    SPC4061 sodium scrambled negative control is the sequence scrambled negative control of SPC4061 sodium.
    SPC4061 sodium scrambled negative control
  • HY-130245A
    (R,R)-PCSK9 degrader 1
    		Degrader
    (R,R)-PCSK9 degrader 1 is the isomer of PCSK9 degrader 1 (HY-130245). 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.
    (R,R)-PCSK9 degrader 1