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    Cryptotanshinone (Cryptotanshinon)
    Cryptotanshinone (Cryptotanshinon)

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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 #: V1383
    CAS #: 35825-57-1Purity ≥98%

    Description: Cryptotanshinone (also called Cryptotanshinon; Tanshinone c), a naturally occuring compound found from the roots of Salvia miltiorrhiza Bunge (Danshen, a Chinese medicinal plant), is a potent STAT3 inhibitor with potential antitumor activity. It inhibits STAT3 with an IC50 of 4.6 μM in a cell-free assay.  

    References: Cancer Res. 2009 Jan 1;69(1):193-202; Mol Pharmacol. 2007 Jul;72(1):62-72. 

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    Molecular Weight (MW)296.36
    FormulaC19H20O3
    CAS No.35825-57-1
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 5 mg/mL (16.9 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)2% DMSO+30% PEG 300+5% Tween 80+ddH2O: 2mg/mL
    SynonymsCryptotanshinon; Tanshinone C.


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    In Vitro

    In vitro activity: Cryptotanshinone, a natural compound isolated from the roots of Salvia miltiorrhiza Bunge (Danshen), significantly inhibits STAT3-dependent luciferase activity, the STAT3 Tyr705 phosphorylation and the dimerization of STAT3, compared to tanshinone IIA which exhibits no activity. Cryptotanshinone (7 μM) dramatically blocks STAT3 Tyr705 phosphorylation but not STAT3 Ser727 phosphorylation in DU145 cells, and significantly inhibits JAK2 phosphorylation with IC50 of ~5 μM without affecting the phosphorylation of upstream kinases c-Src and EGFR, suggesting the inhibition of STAT3 Tyr705 phosphorylation might due to a direct mechanism probably by binding to the SH2 domain of STAT3. Cryptotanshinone significantly inhibits the proliferation of DU145 prostate cancer cells harboring constitutively active STAT3 with GI50 of 7 μM by blocking STAT3 activity, which leads to the down-regulation of cyclin D1, Bcl-xL, and survivin, subsequently the accumulation in the G0-G1 phase. Cryptotanshinone exhibits less growth inhibitory effect on PC3, LNCaP and MDA-MB-468 cells.


    Kinase Assay: HCT-116 cells are transiently transfected with reporter plasmid having the STAT3-binding element for regulating luciferase assay. Cells are treated with Cryptotanshinone for 24 hours at a concentration range of 0.2 to 50 μM. After treatment, cells are harvested in 20 μL of passive lysis buffer and luciferase activity is evaluated by the Dual Luciferase Reporter Assay kit on Wallac Victor2. The concentration of Cryptotanshinone that inhibits the luciferase activity by 50% represents IC50 value.


    Cell Assay: Cells (KATO III, DU145, PC3, LNCaP, MDA-MB-231, MDA-MB-468, MDA-MB-453, MCF-7, MCF-10A, HeLa and HCT-116) are exposed to Cryptotanshinone for 24 or 48 hours. For the determination of cell proliferation, the cell proliferation reagent WST-1 is added and WST-1 formazan is quantitatively measured at 450 nm using an ELISA reader.

    In VivoCryptotanshinone administration significantly reduces the body weight and food intake of ob/ob mice (C57BL/6J-Lepob) and diet-induced obese (DIO) mice in a dose-dependent manner. Cryptotanshinone causes noticeably less fat in the adipose tissues, significant reductions of serum triglycerides and cholesterol levels, and 2.5- to 3-fold higher AMPK activity of the skeletal muscles than in the control mice. Oral administration of Cryptotanshinone at 600 mg/kg/day produces dramatic reductions in blood glucose levels of ob/ob mice (C57BL/6J-Lepob), db/db mice (C57BL/KsJ-Leprdb), and ZDF rats, which occur after 3 days and persist over the entirety of the monitoring period. 
    Animal modelZucker Diabetic Fatty (ZDF) (male) type 2 diabetic rat, ob/ob mice (C57BL/6J-Lepob), db/db mice (C57BL/KsJ-Leprdb) and male C57BL/6J mice with high-fat diet-induced obesity. 
    Formulation & DosageDissolved in 0.1% solution of sodium lauryl sulfate; 600 mg/kg; p.o. 
    References

    Cancer Res. 2009 Jan 1;69(1):193-202; Mol Pharmacol. 2007 Jul;72(1):62-72. 


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

    Cryptotanshinone

    Cryptotanshinone inhibits STAT3-dependent luciferase activity. Cancer Res.2009 Jan 1;69(1):193-202. 
     

    Cryptotanshinone

    Cryptotanshinone sensitively inhibits prostate cancer cells harboring constitutively activated STAT3. Cancer Res. 2009 Jan 1;69(1):193-202. 
     

    Cryptotanshinone

    Cryptotanshinone binds to STAT3 molecules and decreases STAT3 dimerization. Cancer Res. 2009 Jan 1;69(1):193-202.


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