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    Stattic
    Stattic

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V1380
    CAS #: 19983-44-9Purity ≥98%

    Description: Stattic is a small molecule inhibitor of STAT3 that potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM in cell-free assays, it has high selectivity over STAT1. Stattic is the first nonpeptidic small molecule inhibitor of STAT3 with IC50 values of 2.562 ± 0.409 μM, 3.481 ± 0.953 μM, 2.282 ± 0.423 μM and 2.648 ± 0.542 μM, respectively, in UM-SCC-17B, OSC-19, Cal33 and UM-SCC-22B cell lines. Stattic is reported to selectively inhibit dimerization, activation and nuclear translocation of STAT3. It can also induce the apoptosis of STAT3-dependent breast cancer cell lines.

    References: Chem Biol. 2006 Nov;13(11):1235-42; Cancer Res. 2011 May 1;71(9):3182-8. 

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    Molecular Weight (MW)211.19
    FormulaC8H5NO4S
    CAS No.19983-44-9
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 42 mg/mL (198.9 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)2% DMSO+30% PEG 300+H2O: 8 mg/mL
    Synonyms6-Nitro-1-benzothiophene 1,1-dioxide


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    In Vitro

    In vitro activity: Stattic inhibits binding of a phosphotyrosine-containing peptide derived from the gp130 receptor to the STAT3 SH2 domain in a strongly temperature-dependent manner. Stattic only has a very weak effect on binding of a tyrosinephosphorylated peptide to the SH2-domain of the tyrosine kinase Lck. And it doesn’t inhibit dimerization of two other dimeric transcription factors (c-Myc/Max and Jun/Jun). It also inhibits fluorescein-labeled phosphopeptides to the SH2 domains of STAT1 and STAT5b. Stattic selectively inhibits DNA binding of STAT3 homodimers at a concentration of 10 μM. Shown to inhibit cellular phosphorylation of STAT3 at Tyr705 with little effect towards STAT1 phosphorylation at Tyr701 (in HepG2 cells) or the phosphorylation of JAK1, JAK2, and c-Src (in MDA-MB-231 and MDA-MB-235S cells). Stattic increases the apoptotic rate of STAT3-dependent breast cancer cell lines.


    Kinase Assay: Screening is performed at approximately 30 °C. The specificity of screening hits is validated in analogous assays for binding of the test compounds to the SH2 domains of STAT1, STAT5, and Lck. The final concentration of buffer components used for all FP assays is 10 mM HEPES (pH 7.5), 1 mM EDTA, 0.1% Nonidet P-40, 50 mM NaCl, and 10% DMSO. The absence of dithiothreitol is essential for inhibitory activity. The sequences of the peptides are: STAT3, 5-carboxyfluorescein-GY(PO3H2)LPQTV-NH2; STAT1, 5-carboxyfluorescein-GY(PO3H2)DKPHVL; STAT5, 5-carboxyfluorescein-GY(PO3H2)LVLDKW; and Lck, 5-carboxyfluorescein-GY(PO3H2)EEIP. For specificity analysis at 30 °C, proteins are used at 150 nM (STAT1, STAT3, and STAT5). For specificity analysis at 37 °C, proteins are used at 370 nM (STAT3) or 100 nM (Lck). Proteins are incubated with test compounds in Eppendorf tubes at the indicated temperatures for 60 min prior addition of the respective 5-carboxyfluorescein labeled peptides (final concentration: 10 nM). Before measurement at room temperature, the mixtures are allowed to equilibrate for at least 30 min. Test compounds are used at the indicated concentrations diluted from a 20× stock in DMSO. Binding curves and inhibition curves are fitted with SigmaPlot. All competition curves are repeated three times in independent experiment.


    Cell Assay: Stattic significantly inhibited STAT3 activation and expression, leading to decreased cell survival and proliferation as well as increased radiosensitivity. The Stattic treatment also reduced STAT3-mediated HIF-1 expression.

    In VivoIn a murine orthotopic xenograft, oral administration of Stattic effectively reduced the growth of HNSCC tumors, and analysis of tumor lysates validated decreased STAT3 phosphorylation.
    Animal modelUM-SCC-17B cells xenografted mouse model
    Formulation & Dosage50 mg/kg; p.o.
    References

    Cancer Res. 2011 May 1;71(9):3182-8; Chem Biol. 2006 Nov;13(11):1235-42.


    These protocols are for reference only. InvivoChem does not independently validate these methods.

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    STAT3 silencing inhibits the tumor growth of human ABC-like DLBCL Ly3 cells xenografts. Cancer Res. 2011 May 1;71(9):3182-8. 

    Stattic

    STAT3 silencing induces tumor apoptosis and affects infiltration of tumor microenvironment cells in Ly3 xenografts. Cancer Res. 2011 May 1;71(9):3182-8. 
     

    Stattic

    Small-molecule STAT3 inhibitors affect the growth of Ly3 cells in vitro and in vivo. Cancer Res. 2011 May 1;71(9):3182-8. 


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