Catalog Number: 3354
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.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 50 mM in water and to 50 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at RT
  • CAS No:
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.
Additional Information
Licensing Caveats:
Sold for research purposes under agreement from Pfizer Inc.
Background References
  1. Aminopyrrolidineamide inhibitors of site-1 protease.
    Hay et al.
    Bioorg.Med.Chem.Lett., 2007;17:4411
  2. Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease.
    Urata et al.
    J.Virol., 2011;85:795
  3. 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.
    J.Pharmacol.Exp.Ther., 2008;326:801
  4. 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., 2012;8:e1002468

The citations listed below are publications that use Tocris products. Selected citations for PF 429242 include:

Showing Results 1 - 2 of 2

  1. Suppressive effects of the site 1 protease (S1P) inhibitor, PF-429242, on dengue virus propagation.
    Authors: Uchida Et al.
  2. Haploid Genetic Screen Reveals a Profound and Direct Dependence on Cholesterol for Hantavirus Membrane Fusion.
    Authors: Kleinfelter Et al.
    Ann Rheum Dis
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