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NSC 74859 (S3I-201) is a selective Stat3 inhibitor with an IC50 of 86 μM. NSC 74859 (S31-201) is effective in hepatocellular cancers with disrupted TGF-beta signaling.Both CD133 (+) Huh-7 cells and CD133 (-) Huh-7 cells are equally sensitive to NSC 74859 treatment and STAT3 inhibition, with an IC (50) of 100 muM.Furthermore, NSC 74859 (S31-201) treatment of Huh-7 xenografts in nude mice significantly retarded tumor growth, with an effective dose of only 5 mg/kg. Moreover, NSC 74859 (S31-201) inhibited tyrosine phosphorylation of STAT3 in HCC cells in vivo.*The compound is unstable in solutions, freshly prepared is recommended
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Source | Liver Int (2012). Figure 1. NSC 74859 |
| Method | MTT assay | |
| Cell Lines | Non-small cell | |
| Concentrations | 100 μM | |
| Incubation Time | 48 h | |
| Results | Cell viability of hepatoma cells treated with a combination of cetuximab and 100 μM of NSC 74859 decreased significantly, when compared with hepatoma cells treated with cetuximab alone (when the concentration of cetuximab >100 mg/ml, P < 0.0001 for all cell lines) |
| Cell Experiment | |
|---|---|
| Cell lines | NIH 3T3, NIH 3T3/v-Src, MDA-MB-453, MDA-MB-435, MDA-MB-231, or MDA-MB-468 cells line |
| Preparation method | Measurement of Apoptosis by Flow Cytometry. Proliferating cells were treated with or without S3I-201 for up to 48 h. In some cases, cells were first transfected with Stat3C, ST3-NT, or ST3-SH2 domain or mock-transfected for 24 h before treatment with compound for an additional 24-48 h. Cells were then detached and analyzed by annexin V binding (BD Biosciences, San Diego, CA) according to the manufacturer's protocol and flow cytometry to quantify the percent apoptosis. |
| Concentrations | 100 μ M |
| Incubation time | 48 h |
| Animal Experiment | |
|---|---|
| Animal models | Human breast (MDA-MB-231) tumor-bearing mice |
| Formulation | normal saline |
| Dosages | 5 mg/kg every 2 or every 3 days |
| Administration | i.v. |
| Molecular Weight | 365.36 |
| Formula | C16H15NO7S |
| CAS Number | 501919-59-1 |
| Solubility (25°C) | DMSO 80 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related STAT Products |
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| Artesunate
Artesunate is a potential STAT3 inhibitor that acts on the small cell lung cancer cell line H69 with an IC50 value of < 5 μM and is also used in antimalarial studies. Artesunate also promotes ROS signaling and lipid peroxidation by increasing the formation of variable iron pools, ultimately leading to iron death in pancreatic cancer cells. |
| Fludarabine
Fludarabine (NSC 118218) is a STAT1 activation inhibitor and a DNA synthesis inhibitor. Fludarabine inhibits DNA synthesis by interfering with ribonucleotide reductase and DNA polymerase. Fludarabine markedly inhibited VSMC proliferation in cell culture. Fludarabine also induces significant reduction of STAT-1 phosphorylation, whereas it does not change JAK2 activation. Fludarabine exhibits antiproliferative activity (IC50 = 1.54 μM in RPMI cells) and triggers apoptosis through increasing Bax and decreasing Bid, XIAP and survivin expression. |
| Niclosamide
Niclosamide is an inhibitor of STAT3 with an IC50 value of 0.25 μM. |
| Nifuroxazide
Nifuroxazide is a cell-permeable and orally available nitrofuran-based antidiarrheal agent that effectively suppresses the activation of cellular STAT1/3/5 transcription activity with IC50 of 3 μM against IL-6-induced STAT3 activation in U3A cells. |
| Stattic
Stattic is the first nonpeptidic STAT3 inhibitor, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM, highly selectivity over STAT1. Stattic inhibits STAT3 phosphorylation (at Y705 and S727). |
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