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PCSK9

PCSK9 inhibitors and degraders target a secreted protein that limits cholesterol uptake by the liver. Proprotein convertase subtilisin/kexin type 9 (PCSK9) was described in 2003 as neural apoptosis-regulated convertase 1 (NARC-1), a convertase expressed in liver and brain. In the same year, mutations in its gene were linked to autosomal dominant hypercholesterolemia. Secreted PCSK9 binds low-density lipoprotein (LDL) receptors and routes them to lysosomal degradation. SBC-115076 and laroprovstat are small-molecule PCSK9 inhibitors, while PF-06446846 hydrochloride selectively stalls ribosomes during PCSK9 translation. Inclisiran is a small interfering RNA (siRNA), and PCSK9 autophagic degrader 2 removes the protein through autophagy.

2 Items

  • PCSK9 autophagic degrader 2
    Cat. No.
    A46128
    CAS No.
    2974497-11-3

    PCSK9 autophagic degrader 2

    PCSK9 autophagic degrader 2 (W6) targets proprotein convertase subtilisin/kexin type 9 (PCSK9) through an autophagic mechanism, displaying a DC50 value of 20.6 nM. This compound exhibits significant antiatherosclerotic activity, with a dissociation constant (KD) for LC3B of 2.5 μM. PCSK9 autophagic degrader 2 (W6) facilitates research into cholesterol homeostasis, cardiovascular disease, and potential therapeutic interventions targeting the PCSK9 pathway.

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  • (R,R)-PCSK9 degrader 1
    Cat. No.
    A77048
    CAS No.
    2216703-12-5

    (R,R)-PCSK9 degrader 1

    (R,R)-PCSK9 degrader 1 targets proprotein convertase subtilisin/kexin type 9 (PCSK9) and functions as a potent small molecule degrader. With a high affinity (Ki = 107 nM), it effectively disrupts the interaction between PCSK9 and low-density lipoprotein (LDL) receptors. This compound is valuable for research applications focused on cholesterol metabolism and cardiovascular diseases, enabling investigations into the modulation of lipid profiles and potential therapeutic interventions.

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