PF 429242 dihydrochloride
Chemical Name: 4-[(Diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinylbenzamide dihydrochloride
Purity: ≥97%
Biological Activity
PF 429242 dihydrochloride is a 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
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Additional Information
Background References
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Aminopyrrolidineamide inhibitors of site-1 protease.
Hay et al.
Bioorg.Med.Chem.Lett., 2007;17:4411 -
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 -
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 -
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.
Olmstead
PLoS.Pathog., 2012;8:e1002468
Product Datasheets
Citations for PF 429242 dihydrochloride
The citations listed below are publications that use Tocris products. Selected citations for PF 429242 dihydrochloride include:
6 Citations: Showing 1 - 6
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Ambient particulate matter attenuates Sirtuin1 and augments SREBP1-PIR axis to induce human pulmonary fibroblast inflammation: molecular mechanism of microenvironment associated with COPD.
Authors: Tien Et al.
Aging (Albany NY) 2019;11:4654
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A genome-wide CRISPR screen identifies N-acetylglucosamine-1-phosphate transferase as a potential antiviral target for Ebola virus.
Authors: Flint Et al.
Nat Commun 2019;10:285
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TFAP2 transcription factors are regulators of lipid droplet biogenesis.
Authors: Scott Et al.
Elife 2018;7
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Suppressive effects of the site 1 protease (S1P) inhibitor, PF-429242, on dengue virus propagation.
Authors: Uchida Et al.
Viruses 2016;8:E46
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Analysis of Assembly and Budding of Lujo Virus.
Authors: Urata Et al.
J Virol 2015;90:3257
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Haploid Genetic Screen Reveals a Profound and Direct Dependence on Cholesterol for Hantavirus Membrane Fusion.
Authors: Kleinfelter Et al.
Ann Rheum Dis 2015;6:e00801
FAQs
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