PF 429242 dihydrochloride
Chemical Name: 4-[(Diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinylbenzamide dihydrochloride
Biological ActivityPF 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Complete Your Research
Aminopyrrolidineamide inhibitors of site-1 protease.
Hay 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.
Antiviral activity of a small-molecule inhibitor of arenavirus glycoprotein processing by the cellular site 1 protease.
Urata 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.
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
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
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
TFAP2 transcription factors are regulators of lipid droplet biogenesis.
Authors: Scott Et al.
Suppressive effects of the site 1 protease (S1P) inhibitor, PF-429242, on dengue virus propagation.
Authors: Uchida Et al.
Analysis of Assembly and Budding of Lujo Virus.
Authors: Urata Et al.
J Virol 2015;90:3257
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
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