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MedChemExpressModel Nelfinavir -159989-64-7

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Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent[1][2][3].
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Nelfinavir

MCE China:Nelfinavir

Brand:MedChemExpress (MCE)

Cat. No.HY-15287

CAS:159989-64-7

Synonyms:AG1341

Purity:98.83%

Storage:Powder -20°C 3 years 4°C 2 years In solvent -80°C 1 year -20°C 6 months

Shipping:Room temperature in continental US; may vary elsewhere.

Description:Nelfinavir (AG-1341) is a potent and orally bioavailable HIV-1 protease inhibitor (Ki=2 nM) for HIV infection. Nelfinavir is a broad-spectrum, anticancer agent.

In Vitro:Nelfinavir (AG1341) (1-10 μM; 48 hours) inhibits the proliferation of multiple myeloma cells[4]. Nelfinavir inhibits 26S chymotrypsin-like proteasome activity, impairs proliferation and triggers apoptosis of the myeloma cell lines and fresh plasma cells[4]. Nelfinavir (1-10 μM; 17 hours) induces apoptosis of multiple myeloma cell lines[4]. Nelfinavir (5 μM; 0-24 hours) decreases the phosphorylation of AKT[4]. Nelfinavir activates the cleavage of caspase-3, decreases the phosphorylation of AKT, STAT-3, ERK1/2, and activates the pro-apoptotic pathway of the unfolded protein response system[4].

In Vivo:Nelfinavir (AG1341) (75 mg/kg; i.p.; 5 days a week for 21 days) decreases multiple myeloma cell growth in NOD/SCID mice[4].

IC50 & Target:HIV-1

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References:

[1]. Mondal D, et al. Nelfinavir suppresses signaling and nitric oxide production by human aortic endothelial cells: protective effects of thiazolidinediones. Ochsner J. 2013 Spring;13(1):76-90.  [Content Brief]

[2]. Gills JJ, et al. Nelfinavir, A lead HIV protease inhibitor, is a broad-spectrum, anticancer agent that inducesendoplasmic reticulum stress, autophagy, and apoptosis in vitro and in vivo. Clin Cancer Res. 2007 Sep 1;13(17):5183-94.  [Content Brief]

[3]. Kaldor SW, et al. Nelfinavir mesylate (AG1343): a potent, orally bioavailable inhibitor of HIV-1 protease. J Med Chem. 1997 Nov 21;40(24):3979-85.  [Content Brief]

[4]. Bono C, et al. The human immunodeficiency virus-1 protease inhibitor nelfinavir impairs proteasome activity and inhibits the proliferation of multiple myeloma cells in vitro and in vivo. Haematologica. 2012;97(7):1101‐1109.  [Content Brief]

[5]. Qi Sun, et al. Bardoxolone and bardoxolone methyl, two Nrf2 activators in clinical trials, inhibit SARS-CoV-2 replication and its 3C-like protease. Signal Transduct Target Ther. 2021 May 29;6(1):212.  [Content Brief]

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