Cat. No. 3354
Chemical Name: 4-[(Diethylamino)methyl]-N-[2-(2-me
Biological ActivityReversible, competitive inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50 = 0.175 μM). Selective for site 1 protease against a panel of serine proteases. Inhibits rate of cholesterol synthesis in CHO cells (IC50 = 0.53 μM). Also displays antiviral activity. Cell permeable.
Licensing InformationSold for research purposes under agreement from Pfizer Inc.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
Olmstead (2012) 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. PLoS.Pathog. 8 e1002468. PMID: 22241994.
Urata et al (2011) Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease. J.Virol. 85 795. PMID: 21068251.
Hawkins et al (2008) 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.Exp.Ther. 326 801. PMID: 18577702.
Hay et al (2007) Aminopyrrolidineamide inhibitors of site-1 protease. Bioorg.Med.Chem.Lett. 17 4411. PMID: 17583500.
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Citations are publications that use Tocris products. Selected citations for PF 429242 include:
Uchida et al (2016) Suppressive effects of the site 1 protease (S1P) inhibitor, PF-429242, on dengue virus propagation. Viruses 8 E46. PMID: 26875984.
Kleinfelter et al (2015) Haploid Genetic Screen Reveals a Profound and Direct Dependence on Cholesterol for Hantavirus Membrane Fusion. Ann Rheum Dis 6 e00801. PMID: 26126854.
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Keywords: PF 429242, supplier, SREBP, sterol, regulatory, element, binding, proteins, inhibitors, inhibits, site, 1, proteases, S1P, serine, antivirals, PF429242, Tocris Bioscience, SREBP Inhibitor products