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-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.
    Bococizumab
  • HY-132591A
    Inclisiran sodium
    		Inhibitor 98.10%
    Inclisiran sodium is a double-stranded small interfering RNA (siRNA) molecule that inhibits the transcription of PCSK9. Inclisiran sodium can be used for hyperlipidemia and cardiovascular disease (CVD) research.
    Inclisiran sodium
  • 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.
    PF-06446846 hydrochloride
  • HY-132591
    Inclisiran
    		Inhibitor
    Inclisiran (ALN-PCSsc) is a double-stranded small interfering RNA (siRNA) molecule that inhibits the transcription of PCSK9. Inclisiran can be used for hyperlipidemia and cardiovascular disease (CVD) research.
    Inclisiran
  • 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.
    Alirocumab
  • HY-12402
    SBC-115076
    		Inhibitor 99.54%
    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.
    SBC-115076
  • HY-148673
    AZD0780
    		Inhibitor 99.97%
    PCSK9-IN-12 is a heteroaryl compound. PCSK9-IN-12 has bind affinity for PCSK9 with a Kd value of ＜200 nM. PCSK9-IN-12 can be used for the research of cholesterol metabolism.
    AZD0780
  • HY-P2276
    Pep2-8
    		Inhibitor 99.74%
    Pep2-8 is a PCSK9 inhibitor with a binding KD of 0.7 μM and an IC50 of 1.4 μM.
    Pep2-8
  • 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.
    AS-Inclisiran sodium
  • 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.
    Alirocumab (anti-PCSK9)
  • HY-152221
    PCSK9-IN-10
    		Inhibitor 98.95%
    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.
    PCSK9-IN-10
  • 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.
    Anacetrapib
  • 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.
    SS-Inclisiran sodium
  • HY-152223
    PCSK9-IN-11
    		Inhibitor 99.66%
    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 98.42%
    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-P4153
    Enlicitide chloride
    		Inhibitor 98.74%
    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.
    Enlicitide chloride
  • 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.
    5-O-Methylembelin
  • HY-150223
    GalNAc unconjugated/naked Inclisiran
    		Inhibitor
    GalNAc unconjugated/naked Inclisiran is a double-stranded small interfering RNA (siRNA) without GalNAc conjugation. GalNAc unconjugated/naked Inclisiran inhibits the transcription of PCSK-9, and can be used for hyperlipidemia and cardiovascular disease (CVD) research.
    GalNAc unconjugated/naked Inclisiran
  • HY-143220
    SS(no Galnac)-Inclisiran sodium
    		Inhibitor
    SS(no Galnac)-Inclisiran (sodium) is a single stran Inclisiran with no GalNAc. Inclisiran is a double-stranded small interfering RNA (siRNA) molecule that inhibits the transcription of PCSK-9.
    SS(no Galnac)-Inclisiran sodium
  • HY-148687A
    SPC5001 sodium
    		Inhibitor
    SPC5001 sodium is a locked nucleic acid (LNA)-modifed antisense oligonucleotide (ASO) complementary to human PCSK9 (proprotein convertase subtilisin/kexin type 9) mRNA. SPC5001 sodium can be used for the research of hypercholesterolemia. SPC5001 sequence: 5′-TGmCTACAAAACmCmCA-3′.
    SPC5001 sodium