Reversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50
= 0.175 μ
M). Selective for site 1 protease against a panel of serine proteases. Inhibits rate of cholesterol synthesis in CHO cells (IC50
= 0.53 μ
M). Also displays antiviral activity. Cell permeable.
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Aminopyrrolidineamide inhibitors of site-1 protease.
Hay et al.
Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease.
Urata 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.
Hawkins et al.
Human subtilase SKI-1/S1P is a master regulator of the HCV lifecycle and a potential host cell target for developing indirect-acting antiviral agents.
The citations listed below are publications that use Tocris products. Selected citations for PF 429242 include:
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