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    GSK1324726A (I-BET-726)
    GSK1324726A (I-BET-726)

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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 #: V0422
    CAS #: 1300031-52-0Purity ≥98%

    Description: GSK1324726A (I-BET726; GSK-1324726A), a tetrahydroquinoline analog, is a novel and potent ApoA1 up-regulator and selective BET Bromodomain inhibitor with anticancerand anti-inflammatory activity. It inhibits BRD2/3/4 with IC50s of 41 nM, 31 nM, and 22 nM, respectively. It has potent in vitro antiproliferative and anti-inflammatory effects which translate into in vivo efficacy in oncology and inflammation models.  

    References:  2018 Jan 25;61(2):504-513; PLoS One. 2013 Aug 23;8(8):e72967; J Med Chem. 2014 Oct 9;57(19):8111-31.

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    Molecular Weight (MW)434.91
    FormulaC25H23ClN2O3
    CAS No.1300031-52-0
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 86 mg/mL (197.7 mM)
    Water: <1 mg/mL
    Ethanol: 86 mg/mL (197.7 mM)
    SMILESClC1=CC=C(N[[email protected]]2C3=C(C=CC(C4=CC=C(C(O)=O)C=C4)=C3)N(C(C)=O)[[email protected]@H](C)C2)C=C1
    Synonyms

    GSK1324726A, I-BET726, I-BET-726, I-BET 726, GSK-1324726A, GSK 1324726A

    Chemical Name: 4-[(2S,4R)-1-Acetyl-4-[(4-chlorophenyl)amino]-2-methyl-1,2,3,4-tetrahydro-6-quinolinyl]benzoic acid

    Exact Mass: 434.1397 


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    In Vitro

    In vitro activity: In neuroblastoma cell lines, GSK1324726A inhibits cell growth and induces cytotoxicity. GSK1324726A also modulates expression of genes involved in apoptosis, signaling, and MYC-family pathways, including the direct suppression of BCL2 and MYCN.


    Kinase Assay: For determination of binding affinities to BET protein bromodomains, I-BET726 is titrated against truncates containing both BD1 and BD2 of BRD2 (10 nM), BRD3 (10 nM), and BRD4 (10 nM) in 50 mM HEPES pH7.5, 150 mM NaCl, 5% Glycerol, 1 mM DTT and 1 mM CHAPS in the presence of an Alexa 647 derivative (50 nM) of fluorescent ligand. After equilibrating for 1 h, the bromodomain protein: ligand interaction is detected using Time Resolved Fluorescence Resonance Energy Transfer (TR-FRET) following the addition of 1.5 nM europium chelate labeled anti-6His antibody. Plates are read using an Envision Plate reader (λEX = 337 nm, λEM = 615 nm, λEM = 665 nm; dual dichroic = 400 nm & 630 nm). These data are fitted to a four parameter IC50 model using Graphit data analysis software. 


    Cell Assay: Briefly, cells (LA-N-1, Kelly, LA1-55n, BE(2)-M17, BE(2)-C, KanTS, IMR32, LA-N-2, SK-N-SH, SK-N-BE(2), CHP-134, SK-N-AS, SH-SY5Y, SK-N-FI, CHP-212, LA1-5s, SK-N-DZ cells) are seeded into 384-well or 96-well plates at a density optimized for 6 days of growth. The following day, T0 measurements are taken using CellTiter-Glo, CellTiter-Fluor, or CyQuant Direct, following the manufacturer’s instructions. Plates are read on an Envision, Safire 2, or SpectraMax Gemini EM plate reader. Remaining plates are treated with DMSO or a titration of I-BET726. Cells are incubated for 6 days and developed as described above. Results are plotted as a percentage of the T0 value, normalized to 100%, versus concentration of compound. A 4-parameter equation is used to generate concentration response curves. Growth IC50 (gIC50) values are calculated at the mid-point of the growth window (between DMSO and T0 values). Ymin-T0 values are calculated by subtracting the T0 value (100%) from the Ymin value on the curve, and are a measure of net population cell growth or death.

    In VivoIn the mouse SK–N-AS and CHP-212 models, GSK1324726A (15 mg/kg p.o.) results in tumor growth inhibition and down-regulation MYCN and BCL2 expression. In a mouse septic shock model, GSK1324726A (10 mg/kg i.v.) shows potent anti-inflammatory effects, and prevents death of diseased animals
    Animal modelXenograft models of non-MYCN-amplified and MYCN-amplified neuroblastoma in immunocompromised mice using the SK–N-AS and CHP-212 cell lines
    Formulation & DosageSuspended in 1% methylcellulose; 15 mg/kg; p.o.
    References

     PLoS One. 2013 Aug 23;8(8):e72967; J Med Chem. 2014 Oct 9;57(19):8111-31.


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

    GSK1324726A (I-BET726

    I-BET726: a novel selective inhibitor of BET family proteins. . 2013; 8(8): e72967.

    GSK1324726A (I-BET726

    I-BET726 treatment results in potent growth inhibition and cytotoxicity in neuroblastoma cell lines. . 2013; 8(8): e72967.

    GSK1324726A (I-BET726

    Global transcript profiling in neuroblastoma cell lines treated with I-BET726 reveals gene expression changes in apoptotic and signaling pathways. . 2013; 8(8): e72967.

    GSK1324726A (I-BET726

    Suppression of BCL2 expression by I-BET726. . 2013; 8(8): e72967.

    GSK1324726A (I-BET726

    MYCN expression is directly regulated by BRD4 and repressed by treatment with I-BET726. . 2013; 8(8): e72967.

    GSK1324726A (I-BET726

    Analysis of I-BET726 activity in vivo. . 2013; 8(8): e72967.


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