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    SH5-07
    SH5-07

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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 #: V1272
    CAS #: 1456632-41-9Purity ≥98%

    Description: SH5-07 (SH5 07; SH-507; SH5-07), a structural analog of BP-1-102, is a novel, potent and hydroxamic acid-based STAT3 inhibitor with potential antitumor activity. It shows potent anti-proliferative activity in vitro and high in vivo antitumor efficacy against human glioma and breast cancer models. SH5-07 dose-dependently inhibits Stat3 activity with an IC50 of 3.9±0.6 μM in in vitro assay. It preferentially inhibits Stat3: Stat3 DNA-binding activity, ahead of inhibiting Stat1:Stat3 activity, with minimal effects on Stat1:Stat1 activity. SH5-07 binds Stat3, disrupts Stat3 association with growth factor receptor, and thereby inhibits Stat3 phosphorylation. 

    References: Cancer Res. 2016 Feb 1;76(3):652-63.

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    Molecular Weight (MW)625.61 
    FormulaC29H28F5N3O5S 
    CAS No.1456632-41-9 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 100 mg/mL (159.8 mM) 
    Water: <1 mg/mL
    Ethanol: 100 mg/mL (159.8 mM) 
    SMILES O=C(NO)C1=CC=C(N(CC2=CC=C(C3CCCCC3)C=C2)C(CN(C)S(=O)(C4=C(F)C(F)=C(F)C(F)=C4F)=O)=O)C=C1
    Synonyms SH5 07; SH507; SH5-07


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    In Vitro

    In vitro activity: SH5-07 is a hydroxamic acid analog of BP-1-102. SH5-07 dose-dependently inhibits Stat3 activity with an IC50 of 3.9±0.6 μM in in vitro assay. It preferentially inhibits Stat3:Stat3 DNA-binding activity, ahead of inhibiting Stat1:Stat3 activity, with minimal effects on Stat1:Stat1 activity. SH5-07 binds Stat3, disrupts Stat3 association with growth factor receptor, and thereby inhibits Stat3 phosphorylation. It induces antitumor cell effects against malignant cells harboring constitutively-active Stat3. SH5-07 inhibits the expression of known Stat3-regulated genes. Bcl-2, Bcl-xL, c-Myc, Survivin, Cyclin D1 and Mcl-1 expression is reduced in response to 24 h, 5 μM SH5-07 treatment.


    Kinase Assay: SH5-07 is a hydroxamic acid based Stat3 inhibitor with an IC50 of 3.9±0.6 μM in in vitro assay.


    Cell Assay: Cells are treated with 0-8 μM agent for 24-48 h. For cell cycle profile analysis, cells are harvested and fixed with 70% ice-cold ethanol and stained with propidium iodide (PI). For apoptosis analysis, cells are collected and stained with FITC-Annexin V using Apoptosis Detection Kit. Both the DNA content of cells and the Annexin V-positive cells are analyzed by FACScan flow cytometer. Cell cycle phase distribution is analyzed using the Cell-Fit program. Data acquisition is gated to exclude cell doublets

    In VivoTail vein injection or oral gavage delivery of SH5-07 or SH4-54 inhibits growth of 90-150 mm3 established subcutaneous mouse xenografts of human glioma (U251MG) and breast (MDA-MB-231) tumors that harbor aberrantly-active Stat3, associated with decreased c-Myc, Mcl-1 and Cyclin D1 expression. No significant changes in body weights, blood cell counts, or the gross anatomy of organs, or obvious signs of toxicity are observed. 
    Animal modelMouse xenografts with human glioma (U251MG) and breast (MDA-MB-231) tumors
    Formulation & Dosage3, 5 or 6 mg/kg; Oral or tail vein injection
    ReferencesCancer Res. 2016 Feb 1;76(3):652-63 PMC4684502


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

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