1. Epigenetics
  2. Histone Methyltransferase

BIX-01294 (Synonyms: BIX 01294; BIX01294)

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

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10 mM * 1 mL in DMSO $136 In-stock
10 mg $124 In-stock
50 mg $414 In-stock
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Customer Review

Top Publications Citing Use of Products

    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


    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].

    Preparing Stock Solutions
    Concentration Volume (DMSO) 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
    Kinase Assay

    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.

    Cell Assay

    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.





    CAS No.


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

    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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