PF429242 2HCl is a reversible and competitive SREBP site 1 protease (S1P) inhibitor with IC50 value of 175nM.
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PF429242 dihydrochloride is a reversible and competitive inhibitor of SREBP site 1 protease (S1P) with an IC50 of 175 nM[1].
体内研究
In mice treated with PF-429242 for 24 hours, there is a suppression of hepatic SREBP target gene expression, and the rates of cholesterol and fatty acid synthesis in the liver are reduced[1].
体外研究
PF-429242 at 10 μM inhibits endogenous SREBP processing in Chinese hamster ovary cells. It also reduces signaling from an SRE-luciferase reporter gene in human embryonic kidney 293 cells and decreases the expression of endogenous SREBP target genes in HepG2 cells. Additionally, in HepG2 cells, PF-429242 inhibits cholesterol synthesis with an IC50 of 0.5 μM[1].
The addition of PF-429242 at 30 μM significantly suppresses infectious viral titers and viral RNA copies in cell culture fluids. Treatment with PF-429242 also reduces DENV2 yields in the cultured fluids of human-derived HEK-293 and Hep G2 cells, as well as non-human-primate derived LLC-MK2 cells[2].
PF-429242 effectively inhibits the processing of GPC from the prototypic arenaviruses lymphocytic choriomeningitis virus (LCMV) and Lassa virus (LASV). This inhibition correlates with the compound’s potent antiviral activity against LCMV and LASV in cultured cells[3].
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