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    HO-3867
    HO-3867

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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 #: V1384
    CAS #: 1172133-28-6Purity ≥98%

    Description: HO-3867 (HO3867; HO 3867), an analog of curcumin, is a novel, selective and potent STAT3 inhibitor with potential antitumor activity. HO-3867 selectively inhibited STAT3 phosphorylation, transcription, and DNA binding without affecting the expression of other active STATs. O-3867 may be useful to treat ovarian cancer and other solid tumors where STAT3 is commonly upregulated. HO-3867 exhibited minimal toxicity toward noncancerous cells and tissues but induced apoptosis in ovarian cancer cells. Pharmacologic analysis revealed greater bioabsorption and bioavailability of the active (cytotoxic) metabolites in cancer cells compared with normal cells.  

    References: Mol Cancer Ther. 2010 May;9(5):1169-79; Cancer Biol Ther. 2011 Nov 1;12(9):837-45.

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    Molecular Weight (MW)464.55
    FormulaC28H30F2N2O2
    CAS No.1172133-28-6
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 13 mg/mL (28.0 mM)
    Water: <1 mg/mL
    Ethanol: 6 mg/mL (12.9 mM)
    Other infoChemical Name: (3E,5E)-3,5-bis(4-fluorobenzylidene)-1-((1-hydroxy-2,2,5,5-tetramethyl-2,5-dihydro-1H-pyrrol-3-yl)methyl)piperidin-4-one
    InChi Key: PWZQFTQMMAIRRM-JFMUQQRKSA-N
    InChi Code: InChI=1S/C28H30F2N2O2/c1-27(2)15-23(28(3,4)32(27)34)18-31-16-21(13-19-5-9-24(29)10-6-19)26(33)22(17-31)14-20-7-11-25(30)12-8-20/h5-15,34H,16-18H2,1-4H3/b21-13+,22-14+
    SMILES Code: O=C1/C(CN(CC2=CC(C)(C)N(O)C2(C)C)C/C1=C\C3=CC=C(F)C=C3)=C/C4=CC=C(F)C=C4
    SynonymsHO3867; HO 3867; HO-3867


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    In Vitro

    In vitro activity: HO-3867 produces significant cytotoxicity in A2780 and other tested ovarian cancer cell lines, with less toxic to noncancerous ovarian surface epithelial cells. HO-3867 induces G(2)-M cell cycle arrest in A2780 cells and promotes apoptosis by caspase-8 and caspase-3 activation. HO-3867 blocks the JAK/STAT3 pathway in human ovarian cancer cell lines.


    Kinase Assay: HO-3867 is a selective and potent STAT3 inhibitor and shows good antitumor activity.


    Cell Assay: Cell viability is determined by a colorimetric assay using MTT. In the mitochondria of living cells, yellow MTT undergoes a reductive conversion to formazan, producing a purple color. Cells, grown to ~80% confluence in 75-mm flasks, are trypsinized, counted, seeded in 96-well plates with an average population of 7,000 cells/well, incubated overnight, and then treated with HO-3867 for 24 h. All experiments are done using 8 replicates and repeated at least three times.

    In VivoHO-3867 (100 ppm p.o.) inhibits the growth of ovarian cancer xenograft tumor in mice without any apparent signs of toxicity, and also results in inhibition of pSTAT3 as well as downregulation of the STAT3-targeting proteins. HO-3867 sensitizes cisplatin-resistant ovarian carcinoma through STAT3 inhibition. HO-3867 (100 ppm p.o.) also attenuates left-heart-failure-induced pulmonary hypertension by decreasing oxidative stress and increasing PTEN expression in the lung of rats.
    Animal modelMice with ovarian cancer xenograft tumor
    Formulation & Dosage100 ppm p.o.
    ReferencesMol Cancer Ther. 2010 May;9(5):1169-79; Cancer Biol Ther. 2011 Nov 1;12(9):837-45.


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

    HO-3867

    Inhibition of cell viability and proliferation by HO-3867. Mol Cancer Ther. 2010 May;9(5):1169-79. 
     

    HO-3867

    Modulation of cell-cycle progression and cell-cycle regulatory proteins by HO-3867. Mol Cancer Ther.2010 May;9(5):1169-79. 
     

    HO-3867

    Effect of HO-3867 on murine xenograft tumors. Mol Cancer Ther. 2010 May;9(5):1169-79.  
     

    HO-3867

    Induction of apoptosis by HO-3867. Mol Cancer Ther. 2010 May;9(5):1169-79. 
     

    HO-3867

    Inhibition of JAK/STAT3-signaling and downstream proteins by HO-3867. Mol Cancer Ther. 2010 May;9(5):1169-79. 
     

    HO-3867

    Effect of HO-3867 on the expression of JAK/STAT3 and targeting genes. Mol Cancer Ther. 2010 May;9(5):1169-79. 


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