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    BIX 01294
    BIX 01294

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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 #: V0381
    CAS #: 935693-62-2 (free base); Purity ≥98%

    Description: BIX01294 is a novel and potent inhibitor of G9a histone methyltransferase with anticancer activity. It inhibits G9a with an IC50 of 2.7 μM in a cell-free assay. BIX-01294 was discovered by screening a library of 125,000 synthetic and preselected compounds against G9a. It demostrates excellent antiproliferative activity and high in vivo antitumor efficacy. BIX-01294 is selective for G9a and GLP (G9a-like protein) over several H3K9 PKMTs including SUV39H1 and ESET, other KMTs such as SET7/9, and the arginine methyltransferase PRTM1. The X-ray crystal structure of GLP and BIX-01294 confirmed that BIX-01294 bound to the histone peptide binding pocket but failed to interact with the lysine binding channel. 

    References: Mol Cell. 2007 Feb 9;25(3):473-81; J Biol Chem. 2010 May 28;285(22):16538-45.

    Related CAS: 935693-62-2 (free base); 1392399-03-9 (triHCl salt)  

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    Molecular Weight (MW)490.64
    FormulaC28H38N6O2 
    CAS No.935693-62-2 (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 98 mg/mL (163.3 mM)
    Water:  >10 mg/mL 
    Ethanol: 8 mg/mL (13.33 mM)
    SMILESCOC1=C(OC)C=C(C(NC2CCN(CC3=CC=CC=C3)CC2)=NC(N4CCN(C)CCC4)=N5)C5=C1
    SynonymsBIX01294 HCl; BIX01294; BIX-01294; BIX 01294; N-(1-benzylpiperidin-4-yl)-6,7-dimethoxy-2-(4-methyl-1,4-diazepan-1-yl)quinazolin-4-amine 


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    In Vitro

    In vitro activity: BIX01294 is a selective inhibitor of G9a histone methyltransferase and does not affect SUV39H1(H320R) and PRMT1 within the tested concentration range. BIX-01294 specifically inhibited G9a (H3K9me2) and, to a lesser extent, the closely related GLP enzyme (primarily H3K9me3), with an IC50 of 1.7 μM for G9a and 38 μM for GLP. BIX-01294 inhibits G9a in an uncompetitive manner with SAM. BIX-01294 (4.1μM) reduces H3K9me2 Levels in Bulk Histone Preparations from wt ES cells, mouse embryonic fibroblasts and HeLa cells, but not in G9a deficient stem cells. BIX-01294 is a valuable inhibitor for the transient modulation of chromosomal H3K9me2. BIX-01294 Reduces H3K9me2 at Several G9a Target Genes including Bim1 and Serac1. BIX01294 could reactivate expression of HIV-1 from latently infected cells such as ACH-2 and OM10.1


    Kinase Assay: Dissociation Enhanced Lanthanide Fluoro-Immuno Assay (DELFIA) was performed in white, opaque 384-well plates coated with Neutravidin. Test compounds were diluted to 12 μg/mL in 50mM Tris-HCl (pH 8.5) containing 4% DMSO and 10 μL was dispensed into the wells. Blank and control wells received only compound buffer. GST-G9a at 10 μg/mL and SAM at 40 μM were diluted in 50mM Tris HCl (pH 8.5)/10 mM DTT and added in a volume of 20 μL. Blank wells received Tris/DTT buffer only. The reactions were initiated by the addition of 800 nM H3(1-20)-cysbiotin substrate in 50 mM Tris (pH 8.5) in a volume of 10 μL, and incubated at room temperature for 60 mins. The plates were washed 3 times with 100 μL of Wash Buffer. Next, 50 μL of Fluoroimmunoassay (FI) Buffer containing 5 ng α-2X-di-meth H3-K9 and 5 ng goat anti-rabbit Eu chelate was added to all wells of the plate, and the plate was incubated for an additional 1 hr at room temperature. The plates were washed 3 times with 100 μL of Wash Buffer, and 50 μL of Enhancement Solution was added to each well. Time resolved fluorescence was measured after 45 mins on a Viewlux Microplate Imager imaging for 15 seconds.


    Cell Assay: BIX-01294 (4.1 μM) reduced the H3K9me2 Levels in Bulk Histone Preparations from wild-type mouse ES cells, mouse embryonic fibroblasts and human HeLa cells, but not in G9a deficient mouse ES cells.

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    References

    Mol Cell. 2007 Feb 9;25(3):473-81; J Biol Chem. 2010 May 28;285(22):16538-45.


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

    BIX 01294
    Synergistic activation of HIV-1 replication by BIX01294 and SAHA or 5-aza-CdR. J Biol Chem. 2010 May 28; 285(22): 16538–16545.
     



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