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PF-429242 is an inhibitor of site-1 protease with an IC₅₀ value of 170 nM for human recombinant site-1 protease. It is selective for site-1 protease over trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, and furin at concentrations up to 100 μM. PF-429242 completely inhibits proteolytic processing and nuclear translocation of sterol regulatory element-binding protein (SREBP) in HepG2 cells at a concentration of 10 μM. It also reduces expression of HMG-CoA synthase and fatty acid synthase (EC₅₀s = 0.3 and 2 μM, respectively) and inhibits cholesterol synthesis (EC₅₀ = 600 nM) in HepG2 cells and reduces cholesterol and fatty acid synthesis in CD-1 mice. PF-429242 inhibits replication of dengue virus serotypes 1-4 in infected HeLa cells. It also reduces growth of T98G, U87-MG, and A172 glioblastoma cells (IC₅₀s = 0.32, 15.2, and 27.6 μM, respectively).

PF429242 dihydrochloride is a reversible and competitive SREBP site 1 protease (S1P) inhibitor with an IC50 of 175 nM[1].

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[1] Hawkins JL, et al. Pharmacologic inhibition of site 1 protease activity inhibits sterol regulatory element-binding protein processing and reduces lipogenic enzyme gene expression and lipid synthesis in cultured cells and experimental animals. J Pharmacol DOI:10.1124/jpet.108.139626
[2] Uchida L, et al. Suppressive Effects of the Site 1 Protease (S1P) Inhibitor, PF-429242, on Dengue Virus Propagation. Viruses. 2016 Feb 10;8(2). pii: E46. doi: 10.3390/v8020046. DOI:10.3390/v8020046
[3] Urata S, et al. Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J Virol. 2011 Jan;85(2):795-803. DOI:10.1128/JVI.02019-10