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

BIX-01294 trihydrochloride 

Cat. No.: HY-108239
Handling Instructions

BIX-01294 trihydrochloride is a reversible and highly selective G9a Histone Methyltransferase inhibitor, with an IC50 of 2.7 μM in DELFIA assay. BIX-01294 trihydrochloride specifically inhibits G9a (H3K9me2) and GLP enzyme (H3K9me3), with IC50s of 1.7 μM and 38 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.

For research use only. We do not sell to patients.

BIX-01294 trihydrochloride Chemical Structure

BIX-01294 trihydrochloride Chemical Structure

CAS No. : 1392399-03-9

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Top Publications Citing Use of Products

    BIX-01294 trihydrochloride 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

    BIX-01294 trihydrochloride purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2018 Aug 17;37(1):196.

    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.

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    Description

    BIX-01294 trihydrochloride is a reversible and highly selective G9a Histone Methyltransferase inhibitor, with an IC50 of 2.7 μM in DELFIA assay. BIX-01294 trihydrochloride specifically inhibits G9a (H3K9me2) and GLP enzyme (H3K9me3), with IC50s of 1.7 μM and 38 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].

    IC50 & Target

    IC50: 2.7 μM (G9a in DELFIA assay)[2]
    IC50: 1.7 μM for G9a (H3K9me2) and 38 μM for GLP (H3K9me3)[2]
    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].

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

    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].

    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.
    Shipping

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    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    References
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    Keywords:

    BIX-01294 trihydrochloride1392399-03-9Histone MethyltransferaseAutophagyH3K9me2H3K9me3recurrentMLKLp53Cdkn1ap21Gadd45aSUV39H1(H320R)PRMT1Inhibitorinhibitorinhibit

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