pcsk9 in 2

PCSK9-IN-2 is a newly developed small molecule that effectively inhibits the protein-protein interaction (PPI) between PCSK9 and LDLR. It has been found to have a potent inhibitory activity with an IC50 value of 7.57 μM.

PCSK9 modulator-2 (Compound 1) is a potent PCSK9 modulator (EC 50 = 202 nM) with potential applications in hyperlipidemia research. Proprotein convertase subtilisin/kexin type 9 (PCSK9) is a recently validated therapeutic target for lowering low-density lipoprotein cholesterol (LDL-C) [1].

PCSK9 autophagic degrader 2 (W6) is an autophagosome-targeting agent for PCSK9, with a DC50 value of 20.6 nM. It exhibits effects comparable to anti-atherosclerotic treatments and has a binding constant (KD) with LC3B of 2.5 μM.

PCSK9ligand 2 is the target protein ligand of PROTACPCSK9 autophagic degrader 2, and it is applicable for research related to anti-atherosclerosis.

PCSK9-IN-29 serves as a lipid-lowering agent that enhances the expression of low-density lipoprotein receptor (LDLR) protein and reduces PCSK9 protein expression in hepG2 cells. Additionally, in crab-eating macaques on a high-fat diet, it lowers serum LDL-C, TC, and liver enzyme ALT levels, reduces body weight and fat, and boosts bone mineral content. PCSK9-IN-29 is useful for studies involving non-alcoholic fatty liver disease and obesity.

PCSK9-IN-27 (Compound 108) is a PCSK9 inhibitor with an IC50 value of 3.4 nM. It reduces the degradation of LDLR and enhances the uptake of LDL-C.

PCSK9-IN-20 (Compound 3i) is a PCSK9 inhibitor with an IC50 value of 3.96 µM, which reduces PCSK9 and enhances LDLR protein levels in vitro [1].

PCSK9-IN-22 (compound 29), an orally active PCSK9 inhibitor, prevents the protein from interacting with LDLR in vivo [1].

PCSK9-IN-23 (compound 5C), a potent inhibitor of PCSK9, effectively blocks the secretion of PCSK9 from HepG2 cells and significantly enhances the expression of the LDL receptor (LDLR) [1].

PCSK9-IN-26 (Compound 116), an effective PCSK9 inhibitor (IC 50 < 1 nM), is applicable in metabolic research [1].

PCSK9-IN-28 (Compound C11) is a PCSK9 inhibitor that can be isolated from Euphorbia esula. It functions by binding to HNF1α, affecting its nuclear distribution, and thereby inhibiting PCSK9 transcription, which in turn enhances LDLR and promotes LDL uptake. In a high-fat diet (HFD) mouse model, PCSK9-IN-28 demonstrates significant lipid-lowering activity and can be utilized for hyperlipidemia research.

SPC4061, a potent PCSK9 inhibitor and an antisense nucleotide, specifically targets the lock-in nucleic acid (LNA) of PCSK9. This action is relevant for researching hypercholesterolemia and associated diseases [1] [2].

Pep 2-8 ammonium salt is Proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. Potent inhibitor of PCSK9 binding to LDL receptor (IC50 = 0.8 μM). Restores LDL uptake in HepG2 cells treated with PCSK9.