PF 429242

Cat. No. 3354

PF 429242 C25H35N3O2.2HCl [947303-87-9]

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Chemical Name: 4-[(Diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinylbenzamide

Biological Activity

Reversible, 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 Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data

M.Wt:
482.49
Formula:
C25H35N3O2.2HCl
Solubility:
Soluble to 50 mM in water and to 50 mM in DMSO
Purity:
>97 %
Storage:
Desiccate at RT
CAS No:
947303-87-9

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 / Safety Data Sheet

Certificate of Analysis: View current batch
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Safety Data Sheet: View Safety Data Sheet

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.

If you know of a relevant reference for this product please let us know.

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.

Do you know of a great paper that uses PF 429242 from Tocris? If so please let us know.

View Related Products by Product Action

Keywords: PF 429242, supplier, SREBP, sterol, regulatory, element, binding, proteins, inhibitors, inhibits, site, 1, proteases, S1P, serine, antivirals, PF429242, Tocris Bioscience, SREBP Inhibitor products

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