Stattic

Catalog No.S7024 Batch:S702406

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Technical Data

Formula

C8H5NO4S

Molecular Weight 211.19 CAS No. 19983-44-9
Solubility (25°C)* In vitro DMSO 42 mg/mL (198.87 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Add solvents to the product individually and in order)
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O
2.1mg/ml Taking the 1 mL working solution as an example, add 50 μL of 42 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Stattic, the first nonpeptidic small molecule, potently inhibits STAT3 activation and nuclear translocation with IC50 of 5.1 μM in cell-free assays, highly selectivity over STAT1. Stattic induces apoptosis.
Targets
STAT3 [1]
(Cell-free assay)
5.1 μM
In vitro

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. [1]

Features Stattic is the first non-peptide small molecule with inhibitory activity against STAT3 SH2 domain regardless of the STAT3 phosphorylation state in vitro.

Protocol (from reference)

Kinase Assay:

[1]

  • High-Throughput Screening and FluorescencePolarization Assays

    Screening is performed at approximately 30 °C. The specificity ofscreening hits is validated in analogous assays for binding of thetest 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 therespective 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:

[2]

  • Cell lines

    Ly3 cells

  • Concentrations

    ~2.5 μM

  • Incubation Time

    48 h

  • Method

    MTS

Animal Study:

[2]

  • Animal Models

    Ly3 parental NOD/SCID IL2R null xenograft

  • Dosages

    3.75 mg/kg every day

  • Administration

    intra tumor

Customer Product Validation

Data from [Data independently produced by FEBS Lett, 2014, 10.1016/j.febslet.2014.11.023]

Data from [J Biol Chem, 2013, 288(8), 5553-61]

, , Sci Rep, 2017, 7:41404

Data from [Data independently produced by , , Cell Signal, 2017, 32:48-58]

Selleck's Stattic has been cited by 273 publications

Bone morphogenetic protein 4 derived from the cerebrospinal fluid in patients with postherpetic neuralgia induces allodynia via the crosstalk between microglia and astrocyte [ Brain Behav Immun, 2024, 119:836-850] PubMed: 38735405
Bone morphogenetic protein 4 derived from the cerebrospinal fluid in patients with postherpetic neuralgia induces allodynia via the crosstalk between microglia and astrocyte [ Brain Behav Immun, 2024, S0889-1591(24)00395-7] PubMed: 38735405
Cancer-associated fibroblast-derived periostin promotes papillary thyroid tumor growth through integrin-FAK-STAT3 signaling [ Theranostics, 2024, 14(7):3014-3028] PubMed: 38773979
Understanding the molecular pathway of triclosan-induced ADHD-like behaviour: Involvement of the hnRNPA1-PKM2-STAT3 feedback loop [ Environ Int, 2024, 191:108966] PubMed: 39167854
IL-10 protects against OPC ferroptosis by regulating lipid reactive oxygen species levels post stroke [ Redox Biol, 2024, 69:102982] PubMed: 38070317
KRAS/PI3K axis driven GTF3C6 expression and promotes LUAD via FAK pathway [ J Adv Res, 2024, S2090-1232(24)00171-1] PubMed: 38685529
Tumor-associated macrophages drive glycolysis through the IL-8/STAT3/GLUT3 signaling pathway in pancreatic cancer progression [ Cancer Lett, 2024, 588:216784] PubMed: 38458594
Malat1 regulates PMN-MDSC expansion and immunosuppression through p-STAT3 ubiquitination in sepsis [ Int J Biol Sci, 2024, 20(4):1529-1546] PubMed: 38385073
Hypoxia-induced miR-5100 promotes exosome-mediated activation of cancer-associated fibroblasts and metastasis of head and neck squamous cell carcinoma [ Cell Death Dis, 2024, 15(3):215] PubMed: 38485986
The microglial innate immune protein PGLYRP1 mediates neuroinflammation and consequent behavioral changes [ Cell Rep, 2024, 43(3):113813] PubMed: 38393947

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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