2. Epigenetics Autophagy
  3. Histone Methyltransferase Autophagy
  4. BIX-01294 trihydrochloride

BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells.

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BIX-01294 trihydrochloride Chemical Structure

BIX-01294 trihydrochloride Chemical Structure

CAS No. : 1392399-03-9

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BIX-01294 trihydrochloride Related Antibodies

Top Publications Citing Use of Products

    BIX-01294 trihydrochloride 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 trihydrochloride 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 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

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    Description

    BIX-01294 trihydrochloride is a reversible and highly selective G9a and GLP Histone Methyltransferase inhibitor, with IC50s of of 1.7 μM and 0.9 μM, respectively. BIX-01294 trihydrochloride inhibits G9a/GLP by competing for binding with the amino acids N-terminal of the substrate lysine residue. BIX-01294 trihydrochloride, a (1H-1,4-diazepin-1-yl)-quinazolin-4-yl amine derivative, induces necroptosis and autophagy. BIX-01294 trihydrochloride has antitumor activity in recurrent tumor cells[1][2][3][4][5].

    IC50 & Target

    IC50: 2.7 μM (G9a in DELFIA assay)[2]
    IC50: 1.9 μM for G9a and 0.7 μM for GLP[5]
    In Vitro

    BIX-01294 (2 μM; 48 h) trihydrochloride selectively inhibits recurrent tumor cell growth[1].
    BIX-01294 (1 μM) trihydrochloride leads to a marked increase in phosphorylation of S345 of MLKL[1].
    BIX-01294 (1 μM) trihydrochloride significantly upregulates the canonical p53 targets Cdkn1a (p21) and Gadd45a in recurrent tumor cell lines[1].
    BIX-01294 (1 μM; 6 days) trihydrochloride causes the reduction in H3K9me2 levels in primary and recurrent tumor cells[1].
    BIX-01294 trihydrochloride leads to necroptotic cell death in recurrent tumor cells. Necrostatin-1 (30 μM) partially reverses cell death induced by BIX-01294 (750 nM; 24 h) trihydrochloride[1].
    BIX-01294 (4.1 μM; for 2 days) trihydrochloride causes around a 20% reduction, concomitant with a comparable increase in the unmodified H3K9 fragment in H3K9me2 in mouse ES cells. BIX-01294 trihydrochloride causes pronounced reduction in H3K9me2 and a small decrease for H3K9me3 and H3K9me1 in wild-type ES cells[2].
    BIX-01294 trihydrochloride has no inhibition of the other histone methyltransferases even at concentrations of 45 μM. BIX-01294 trihydrochloride does not affect SUV39H1 (H320R) and PRMT1 within the tested concentration range (up to 10 μM)[2].
    BIX-01294 trihydrochloride inhibits G9a in an uncompetitive manner with S-adenosyl-methionine (SAM)[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].

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

    BIX-01294 trihydrochloride Related Antibodies

    Cell Viability Assay[1]

    Cell Line: Primary or recurrent tumor cells
    Concentration: 2 μM
    Incubation Time: 48 h
    Result: Selectively inhibited recurrent tumor cell growth.
    In Vivo

    BIX-01294 trihydrochloride (10 mg/kg; IP; three times a week for 2 weeks) significantly reduces tumor growth and tumor burden in recurrent tumor cells. Primary tumor growth is not inhibited[1].

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

    Animal Model: Female MMTV-rtTA;TetO-Her2/neu (MTB;TAN) and TetO-Her2/neu (TAN) mice with recurrent or primary tumor cells[1]
    Dosage: 10 mg/kg
    Administration: IP; three times a week for 2 weeks
    Result: Significantly reduced tumor growth and tumor burden in recurrent tumor cells.
    Primary tumor growth was not inhibited.
    Slowed the growth of orthotopic recurrent tumors in athymic nude recipients.
    Molecular Weight

    600.02

    Formula

    C28H41Cl3N6O2
    CAS No.
    SMILES

    CN(CCC1)CCN1C2=NC(C=C(OC)C(OC)=C3)=C3C(NC4CCN(CC5=CC=CC=C5)CC4)=N2.Cl.Cl.Cl
    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 trihydrochloride 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 trihydrochloride1392399-03-9Histone MethyltransferaseAutophagyH3K9me2H3K9me3recurrentMLKLp53Cdkn1ap21Gadd45aSUV39H1(H320R)PRMT1Inhibitorinhibitorinhibit

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