A site-1 protease inhibitor (IC50 =170 nM against human recombinant site-1 protease); selective for site-1 protease over trypsin

PF-429242 (hydrochloride) – 5 mg

Brand:
Cayman
CAS:
2248666-66-0
Storage:
-20
UN-No:
De Minimis - 3077 / 9

PF-429242 is an inhibitor of site-1 protease with an IC50 value of 170 nM for human recombinant site-1 protease.{38306} It is selective for site-1 protease over trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, and furin at concentrations up to 100 μM. PF-429242 completely inhibits proteolytic processing and nuclear translocation of sterol regulatory element-binding protein (SREBP) in HepG2 cells at a concentration of 10 μM. It also reduces expression of HMG-CoA synthase and fatty acid synthase (EC50s = 0.3 and 2 μM, respectively) and inhibits cholesterol synthesis (EC50 = 600 nM) in HepG2 cells and reduces cholesterol and fatty acid synthesis in CD-1 mice. PF-429242 inhibits replication of dengue virus serotypes 1-4 in infected HeLa cells.{38307} It also reduces growth of T98G, U87-MG, and A172 glioblastoma cells (IC50s = 0.32, 15.2, and 27.6 μM, respectively).{38308}  

 

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Description

A site-1 protease inhibitor (IC50 =170 nM against human recombinant site-1 protease); selective for site-1 protease over trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, and furin at concentrations up to 100 μM; inhibits proteolytic processing and nuclear translocation of SREBP; reduces expression of HMG-CoA synthase and fatty acid synthase (EC50s = 0.3 and 2 μM, respectively) and inhibits cholesterol synthesis (EC50 = 600 nM) in HepG2 cells; reduces cholesterol and fatty acid synthesis in CD-1 mice; inhibits replication of dengue virus serotypes 1-4 in infected HeLa cells; reduces growth of T98G, U87-MG, and A172 glioblastoma cells (IC50s = 0.32, 15.2, and 27.6 μM, respectively),

Formal name: 4-[(diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinyl-benzamide, dihydrochloride

Synonyms: 

Molecular weight: 482.5

CAS: 2248666-66-0

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Antivirals||Product Type|Biochemicals|Small Molecule Inhibitors|Peptidases & Proteases||Research Area|Cancer||Research Area|Immunology & Inflammation||Research Area|Infectious Disease|Viral Diseases|Dengue

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