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SH-4-54 is a potent STAT inhibitor with KD values of 300 nM and 464 nM for STAT3 and STAT5, respectively. SH-4-54 potently kills glioblastoma brain cancer stem cells (BTSCs) and effectively suppresses STAT3 phosphorylation and its downstream transcriptional targets at low nM concentrations. SH-4-54 exhibites blood-brain barrier permeability, potently controlled glioma tumor growth, and inhibites pSTAT3 in vivo.
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Source | Int J Mol Sci (2018). Figure 4. SH-4-54 |
| Method | cell viability assay | |
| Cell Lines | LX-2 and HSC-T6 | |
| Concentrations | 1.5 μM or 0.5 μM | |
| Incubation Time | 48 h | |
| Results | A second STAT3 specific inhibitor, SH-4-54, inhibited LX-2 cell viability in a dose-dependent manner with an IC50 of 0.37 μM. |
| Cell Experiment | |
|---|---|
| Cell lines | BTSC lines 25M, 67EF, 73EF, 84EF and 127EF |
| Preparation method | Dissociating BTSC spheres to single cells with the enzyme Accumax, seeding at 1500 cells/ 96-well and treating with drug or vehicle (DMSO) one day after plating. Repeating cytotoxicity studies independently using BTSC lines 25M, 67EF, 73EF, 84EF and 127EF.Dissociating BTSC spheres to single cells as above and plating in 96 well plates in triplicate at 3000 cells/ 96-well. In both sets of experiments using drugs as serial dilutions within the range of 5 μM to 100 nM in the first set and 25 μM to 10 nM. Assessing cell viability following drug treatment three days later using the alamarBlue assay according to the manufacturer’s instructions. All culture experiments are performed in triplicate with a minimum of three wells per condition |
| Concentrations | ~25 μM |
| Incubation time | 72 hours |
| Animal Experiment | |
|---|---|
| Animal models | NOD-SCID bearing ed with BT73 glioma xenografts |
| Formulation | 10 mg/kg |
| Dosages | Suspended in 50% polyethylene glycol 300 in water |
| Administration | i.p. |
| Molecular Weight | 610.59 |
| Formula | C29H27F5N2O5S |
| CAS Number | 1456632-40-8 |
| 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 |
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| 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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