PF 429242 - CAS 947303-87-9
Catalog number: 947303-87-9
Category: Inhibitor
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Molecular Formula:
C25H35N3O2
Molecular Weight:
409.56
COA:
Inquire
Targets:
Others
Description:
PF 429242 is a reversible, competitive, cell permeable inhibitor of sterol regulatory element-binding protein (SREBP) site 1 protease (IC50 = 0.175 μM) without disrupting a panel of serine proteases. Some studies reported that the inhibition of SKI-1/S1P, a master lipo- 387 genic regulator, could impair HCV genome replication, lipid droplet 388 homeostasis and the production of infectious HCV virions.
Brife Description:
A competitive inhibitor of SREBP site 1 protease (IC50 = 0.175 μM)
Appearance:
White solid
Synonyms:
PF-429242; PF 429242; PF429242. Benzamide, 4-​[(diethylamino)​methyl]​-​N-​[2-​(2-​methoxyphenyl)​ethyl]​-​N-​(3R)​-​3-​pyrrolidinyl-; 4-[(Diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinylbenzamide
Solubility:
Soluble to 50 mM in water and to 50 mM in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -42℃ for long term (months to years).
MSDS:
Inquire
Shelf Life:
2 years
Boiling Point:
562.2±50.0 °C | Condition: Press: 760 Torr
Density:
1.11±0.1 g/cm3
InChIKey:
XKPJTOHUPQWSOJ-HSZRJFAPSA-N
InChI:
1S/C25H35N3O2/c1-4-27(5-2)19-20-10-12-22(13-11-20)25(29)28(23-14-16-26-18-23)17-15-21-8-6-7-9-24(21)30-3/h6-13,23,26H,4-5,14-19H2,1-3H3/t23-/m1/s1
Canonical SMILES:
CCN(CC)CC1=CC=C(C=C1)C(=O)N(CCC2=CC=CC=C2OC)C3CCNC3
1.Suppressive Effects of the Site 1 Protease (S1P) Inhibitor, PF-429242, on Dengue Virus Propagation.
Uchida L1, Urata S2, Ulanday GE3,4, Takamatsu Y5, Yasuda J6,7, Morita K8,9, Hayasaka D10,11. Viruses. 2016 Feb 10;8(2). pii: E46. doi: 10.3390/v8020046.
Dengue virus (DENV) infection causes one of the most widespread mosquito-borne diseases in the world. Despite the great need, effective vaccines and practical antiviral therapies are still under development. Intracellular lipid levels are regulated by sterol regulatory elements-binding proteins (SREBPs), which are activated by serine protease, site 1 protease (S1P). Small compound PF-429242 is known as a S1P inhibitor and the antivirus effects have been reported in some viruses. In this study, we examined the anti-DENV effects of PF-429242 using all four serotypes of DENV by several primate-derived cell lines. Moreover, emergence of drug-resistant DENV mutants was assessed by sequential passages with the drug. DENV dependency on intracellular lipids during their infection was also evaluated by adding extracellular lipids. The addition of PF-429242 showed suppression of viral propagation in all DENV serotypes. We showed that drug-resistant DENV mutants are unlikely to emerge after five times sequential passages through treatment with PF-429242.
2.SKI-1/S1P inhibitor PF-429242 impairs the onset of HCV infection.
Blanchet M1, Sureau C2, Guévin C1, Seidah NG3, Labonté P4. Antiviral Res. 2015 Mar;115:94-104. doi: 10.1016/j.antiviral.2014.12.017. Epub 2015 Jan 5.
Worldwide, approximately 170 million individuals are afflicted with chronic hepatitis C virus (HCV) infection. To prevent the development of inherent diseases such as cirrhosis and hepatocellular carcinoma, tremendous efforts have been made, leading to the development of promising new treatments. However, their efficiency is still dependent on the viral genotype. Additionally, these treatments that target the virus directly can trigger the emergence of resistant variants. In a previous study, we have demonstrated that a long-term (72h) inhibition of SKI-1/S1P, a master lipogenic pathway regulator through activation of SREBP, resulted in impaired HCV genome replication and infectious virion secretion. In the present study, we sought to investigate the antiviral effect of the SKI-1/S1P small molecule inhibitor PF-429242 at the early steps of the HCV lifecycle. Our results indicate a very potent antiviral effect of the inhibitor early in the viral lifecycle and that the overall action of the compound relies on two different contributions.
3.Evaluation of the anti-arenaviral activity of the subtilisin kexin isozyme-1/site-1 protease inhibitor PF-429242.
Pasquato A1, Rochat C, Burri DJ, Pasqual G, de la Torre JC, Kunz S. Virology. 2012 Feb 5;423(1):14-22. doi: 10.1016/j.virol.2011.11.008. Epub 2011 Dec 10.
The cellular protease subtilisin kexin isozyme-1 (SKI-1)/site-1 protease (S1P) is implicated in the proteolytic processing of the viral envelope glycoprotein precursor (GPC) of arenaviruses, a step strictly required for production of infectious progeny. The small molecule SKI-1/S1P inhibitor PF-429242 was shown to have anti-viral activity against Old World arenaviruses. Here we extended these studies and show that PF-429242 also inhibits GPC processing and productive infection of New World arenaviruses, making PF-429242 a broadly active anti-arenaviral drug. In combination therapy, PF-429242 potentiated the anti-viral activity of ribavirin, indicating a synergism between the two drugs. A hallmark of arenaviruses is their ability to establish persistent infection in vitro and in vivo. Notably, PF-429242 was able to efficiently and rapidly clear persistent infection by arenaviruses. Interruption of drug treatment did not result in re-emergence of infection, indicating that PF-429242 treatment leads to virus extinction.
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CAS 947303-87-9 PF 429242

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