A site-1 protease inhibitor
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PF-429242 (hydrochloride)

Item No. 15140

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
4-[(diethylamino)methyl]-N-[2-(2-methoxyphenyl)ethyl]-N-(3R)-3-pyrrolidinyl-benzamide, dihydrochloride
CAS Number
2248666-66-0
Molecular Formula
C25H35N3O2 • 2HCl
Formula Weight
482.5
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMSO: 30 mg/mlEthanol: 30 mg/mlPBS (pH 7.2): 10 mg/ml
λmax
272 nm
SMILES
O=C(C1=CC=C(CN(CC)CC)C=C1)N(CCC2=CC=CC=C2OC)[C@H]3CNCC3.Cl.Cl
InChi Code
InChI=1S/C25H35N3O2.2ClH/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;2*1H/t23-;;/m1../s1
InChi Key
GSUZWFZKTIOWTI-MQWQBNKOSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    PF-429242 is an inhibitor of site-1 protease with an IC50 value of 170 nM for human recombinant site-1 protease.1 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.2 It also reduces growth of T98G, U87-MG, and A172 glioblastoma cells (IC50s = 0.32, 15.2, and 27.6 μM, respectively).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Hay, B.A., Abrams, B., Zumbrunn, A.Y., et al. Aminopyrrolidineamide inhibitors of site-1 protease. Bioorg. Med. Chem. Lett. 17(16), 4411-4414 (2007).

    2. Uchida, L., Urata, S., Ulanday, G.E., et al. Suppressive effects of the site 1 protease (S1P) inhibitor, PF-429242, on Dengue virus propagation. Viruses 8(2), 46 (2016).

    3. Caruana, B.T., Skoric, A., Brown, A.J., et al. Site-1 protease, a novel metabolic target for glioblastoma. Biochem. Biophys. Res. Commun. 490(3), 760-766 (2017).