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    INH1 (IBT13131)
    INH1 (IBT13131)

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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 #: V1614
    CAS #: 313553-47-8Purity ≥98%

    Description: INH1 (also called IBT-13131; INH-1; IBT13131) is a potent and cell-permeable Hec1 (High expression in cancer 1) inhibitor with potential anticancer activity. It acts by specifically disrupting the Hec1/Nek2 protein-protein interaction.  

    References: Cancer Res. 2008 Oct 15;68(20):8393-9.

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    Molecular Weight (MW)308.40 
    FormulaC18H16N2OS 
    CAS No.313553-47-8 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 61 mg/mL (197.8 mM) 
    Water: <1 mg/mL
    Ethanol: 61 mg/mL (197.8 mM) 
    SMILESO=C(NC1=NC(C2=CC=C(C)C=C2C)=CS1)C3=CC=CC=C3
    SynonymsIBT-13131; INH-1; IBT 13131; INH 1; IBT13131; INH1 


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    In Vitro

    In vitro activity: INH1 reduces the association of Hec1 with kinetochore and decreases global Nek2 protein level in cells. INH1 effectively inhibits the proliferation of human breast cancer lines with GI50 of 10-21 μM. Moreover, INH1 also elicits cell killing activity in part through impairing the Hec1/Nek2 pathway for the spindle checkpoint regulation.


    Kinase Assay: Surface plasma resonance (SPR) assays are performed at 22.5°C in HBSD buffer [10 mmol/L HEPES, 150 mmol/L NaCl, 0.1% DMSO (pH 7.5)] on Biacore 3000. 6×His-Hec1 and GST-Nek2 are purified. NTA sensor chip or glutathione-modified CM5 chip are used to capture His-Hec1 and GST-Nek2, respectively. The capture level is about 140 to 180 resonance units (RU) at the flow rate of 5 μL/min. For the binding assay, chips are sequentially treated with compounds (1 or 20 μmol/L) and then proteins (50 μg/mL). Retained RUs are recorded and processed (triplicate experiments). 


    Cell Assay: Standard 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assays with a 3-d drug treatment procedure are performed to measure the dose-dependent cytotoxicity of INH1 in cultured cells. Triplicate sets are measured and compiled for final data presentation. Cell lines used: MDA-MB-468, SKBR3, T47D, MDA-MB-361, ZR-75-1, HBL100, MDA-MB-435, HS578T, and MCF10A cells.

    In VivoINH1 (100 mg/kg i.p.) inhibits breast tumor growth in mice bearing MDA-MB-468 human breast cancer xenograft. 
    Animal modelAthymic female BALB/c nude mice bearing MDA-MB-468 human breast cancer xenografts. 
    Formulation & DosageDissolved in 15% DMSO, 20% Tween 20, 10% PEG-400, 55% saline; 100 mg/kg; i.p. injection 
    References

    Cancer Res. 2008 Oct 15;68(20):8393-9. 


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

    INH1

    INH1 treatment triggered Nek2 reduction and defective Hec1 localization on kinetochores. Cancer Res. 2008 Oct 15;68(20):8393-9.
     

    INH1

    Cancer Res. 2008 Oct 15;68(20):8393-9.
     

    INH1

    J Med Chem. 2009 Mar 26;52(6):1757-67.


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