The small molecule PF-429242 was developed as a hypolipidemic agent based on high throughput screening in a Pfizer compound library. PF-429242 is a competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50 = 0.175 uM). It is selective for site 1 protease against a panel of serine proteases. PF-429242 inhibits rate of cholesterol synthesis in CHO cells (IC50 = 0.53 uM). PF-429242 inhibits the activity of S1P reversibly and competitively and suppresses the expression level of SREBP target genes, consequently decreasing cellular lipid levels. It has been shown that PF-429242 suppresses hepatic SREBP target genes and inhibits cholesterol and fatty acid synthesis in a mouse model. It also has been reported that PF-429242 suppresses viral replication in cells infected with hepatitis C virus (HCV), Lassa virus, lymphocytic choriomeningitis virus, New World arenaviruses and Dengue virus.