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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.
| Cell Experiment | |
|---|---|
| Cell lines | SKM-1 cells |
| Preparation method | Growth inhibition assay: The SKM-1 cells (1×105/mL) are firstly seeded in 96-well plates. Artesunate is diluted in 0.1% dimethyl sulfoxide (DMSO) producing 0, 12.5, 25, 50µg/mL concentrations and added to the SKM-1 cells with 100 µl per well. A negative control is treated with 0.1% DMSO. At 0, 24, 48, and 72 hours, same amount of MTT solution is added into each well and cultured for extra 4 hours. MTT treated cells are fixed with 150 µL DMSO for 30 min at room temperature and then determined with Evolution 201 and 220 UV-Vis spectrophotometer system at 540 nm. |
| Concentrations | 0, 12.5, 25, 50 µg/mL |
| Incubation time | 0, 24, 48, and 72 h |
| Animal Experiment | |
|---|---|
| Animal models | BALB/c mice |
| Formulation | Dissolved in DMSO and diluted with sterile PBS |
| Dosages | 100 mg/kg/day |
| Administration | i.p. |
| Molecular Weight | 384.42 |
| Formula | C19H28O8 |
| CAS Number | 88495-63-0 |
| Solubility (25°C) | DMSO: ≥ 60 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 |
|---|
| NSC 74859 (S3I-201)
NSC 74859 (S3I-201) is a selective Stat3 inhibitor with an IC50 of 86 μM. NSC 74859 (S3I-201) is effective in hepatocellular cancers with disrupted TGF-beta signaling.*The compound is unstable in solutions, freshly prepared is recommended |
| 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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