1. Epigenetics
    Autophagy
  2. Histone Methyltransferase
    Autophagy

BIX-01294 

Cat. No.: HY-10587 Purity: 99.22%
Data Sheet SDS Handling Instructions

BIX-01294 is an inhibitor of G9a Histone Methyltransferase with IC50 of 1.9 μM.

For research use only. We do not sell to patients.
BIX-01294 Chemical Structure

BIX-01294 Chemical Structure

CAS No. : 935693-62-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO $136 In-stock
10 mg $124 In-stock
50 mg $414 In-stock
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

    BIX-01294 purchased from MCE. Usage Cited in: Cell Death Dis. 2017 Apr 6;8(4):e2726.

    Upper and middle panels: WB detection of H3K9me2 and G9A in PC9 and A549 cells treated with 0, 1, 2.5, 5 or 10 μM BIX-01294. The total level of histone H3 and actin serve as loading controls. Lower panel: WB detection of the total (T-) level of and phosphorylated (P-) ERK kinase in PC9 and A549 cells treated with 0, 1, 5 or 10 μM BIX-01294. GAPDH serves as the loading control
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    BIX-01294 is an inhibitor of G9a Histone Methyltransferase with IC50 of 1.9 μM.

    IC50 & Target

    IC50: 1.9 μM (G9a Histone Methyltransferase)

    In Vitro

    BIX-01294 (4.1 μM) treatment of G9anull ES cells results in a further reduction in H3K9me2 levels. BIX-01294 reduces H3K9me2 at several G9a target genes[1]. BIX-01294 (5 µM) reduces levels of global H3K9 methylation in pronuclear- and 2-cell-stage embryos. Embryos transiently exposed to BIX-01294 have a reduced ability to establish pregnancy[2]. BIX-01294 (1 µg/mL) causes reduction in the BrdU incorporation of fetal PASMCs. BIX-01294 treatment decreases the PASMCs migration induced by PDGF[3].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.0382 mL 10.1908 mL 20.3815 mL
    5 mM 0.4076 mL 2.0382 mL 4.0763 mL
    10 mM 0.2038 mL 1.0191 mL 2.0382 mL
    Please refer to the solubility information to select the appropriate solvent.
    Kinase Assay
    [1]

    Test compounds are diluted to 12 μg/mL in 50 mM Tris-HCl pH 8.5 containing 4% DMSO and 10 μL is dispensed into the wells. Blank and control wells receive only compound buffer. GST-G9a at 10 μg/mL and SAM at 40 μM are diluted in 50 mM Tris HCl pH 8.5/10 mM DTT and added in a volume of 20 μL. Blank wells receive Tris/DTT buffer only. The reactions are 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 minutes. The plates are washed 3 times with 100 μL of ish Buffer (50 mM Tris pH 7.4, 150 mM NaCl, 0.05% Tween 20, 0.2% BSA). Next, 50 μL of luoroimmunoassay (FI) Buffer (50 mM Tris HCl pH 7.8, 150 mM NaCl, 0.05% Tween 40, 25 μM DTPA, 0.2% BSA, 0.05% BGG) containing 5 ng α-2X-di-meth H3-K9 and 5 ng goat anti-rabbit Eu chelate is added to all wells of the plate, and the platei s incubated for an additional hour at room temperature. The plates are washed 3 times with 100 μL of ish Buffer, and 50 μL of Enhancement Solution is added to each well. Time resolved fluorescence is measured after 45 minutes on a Viewlux Microplate Imager imaging for 15 seconds with a 354 μs window, 400 μs delay, excitation at 360 nm, and emission at 618 nm. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Cell Assay
    [3]

    Briefly, fetal PASMCs are plated in 96-well plates and starved for 24 h at 0.1% serum containing medium. PDGF-BB is added for 24 h at the indicated concentrations in the presence or absence of BIX-01294. BrdU label solution is added to each well 18 h prior to analysis. Denaturing solution is added to each well for 30 min at room temperature after removing the contents of wells. Then, anti-BrdU antibody is added to each well and incubated for 1 h and peroxidase goat anti-mouse IgG HRP conjugate is added in the well for 30 min at room temperature. The absorbance is read at 450-540 nm on a Glomax Multiple Detection System. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    490.64

    Formula

    C₂₈H₃₈N₆O₂

    CAS No.

    935693-62-2

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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    Inquiry Information

    Product Name:
    BIX-01294
    Cat. No.:
    HY-10587
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