2. Epigenetics Apoptosis Autophagy
  3. Histone Methyltransferase Apoptosis Autophagy
  4. BIX-01294 hydrochloride hydrate

BIX-01294 hydrochloride hydrate is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC50 of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells.

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BIX-01294 hydrochloride hydrate Chemical Structure

BIX-01294 hydrochloride hydrate Chemical Structure

CAS No. : 1808255-64-2

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BIX-01294 hydrochloride hydrate Related Antibodies

Top Publications Citing Use of Products

    BIX-01294 hydrochloride hydrate purchased from MedChemExpress. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 17;37(1):196.  [Abstract]

    The relative mRNA levels of Ki67 and PCNA in primary CRC cells responding to rhIL-33 (100 ng/mL) incubation and/ or indicated inhibitors (SB203580, 10 μg/mL; PD98059, 20 μg/mL; SP600125, 10 μg/mL; BIX01294, 2 μM; 5Aza, 10 μM; SC560, 0.1 μg/mL; celecoxib, 20 μg/mL) for 24 h.

    BIX-01294 hydrochloride hydrate purchased from MedChemExpress. Usage Cited in: Cell Death Dis. 2017 Apr 6;8(4):e2726.  [Abstract]

    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

    View All Histone Methyltransferase Isoform Specific Products:

    View All Isoforms
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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    Description

    BIX-01294 hydrochloride hydrate is a histone-lysine methyltransferase (HMTase) inhibitor, which selective inhibits the G9aHMTase with IC50 of 1.7 μM, reduces histone-3 lysine (9) methylation (H3K9me), induces autophagy and apoptosis in human glioma cells[1][2].

    IC50 & Target

    G9a

    1.7 μM (IC50)

    GLP

    38 μM (IC50)

    In Vitro

    BIX-01294 hydrochloride hydrate (1–10 μM) induces autophagy and apoptosis and reduces cell viability in LN18 glioma cells[1]. BIX-01294 hydrochloride hydrate (1–10 μM) upregulates levels of autophagy-related genes LC3B, WIPI1 and downregulates the differentiation-related genes GFAP, TUBB3, results in an autophagy-dependent differentiation in glioma stem-like cells (GSC)[1].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    BIX-01294 hydrochloride hydrate Related Antibodies

    Cell Viability Assay[1]

    Cell Line: LN18
    Concentration: 1–10 μM
    Incubation Time: 24-72 h
    Result: Reduced cell viability of LN18 in a dose-dependent manner.

    Western Blot Analysis[1]

    Cell Line: LN18
    Concentration: 1–10 μM
    Incubation Time: 24-72 h
    Result: Increased levels of cleaved caspase3/7 and cleaved PARP. Decreased levels of H3K9me2, H3K27me3 and accumulation of LC3-II.
    Formula

    C28H38N6O2.3ClH.xH2O
    CAS No.
    SMILES

    COC1=CC2=C(NC3CCN(CC3)CC4=CC=CC=C4)N=C(N5CCN(CCC5)C)N=C2C=C1OC.Cl.O.Cl.Cl.[x]
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
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    BIX-01294 hydrochloride hydrate Related Classifications

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    BIX-01294 hydrochloride1808255-64-2Histone MethyltransferaseApoptosisAutophagygliomahistone methyltransferaseInhibitorinhibitorinhibit

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