pcsk9in2

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-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.