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

BIX-01294 trihydrochloride 

目录号: HY-108239 纯度: 99.68%
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BIX-01294 trihydrochloride 是一种可逆且高度选择性的 G9a 和 GLP 组蛋白甲基转移酶抑制剂，IC50 分别为 1.9 μM 和 0.7 μM。BIX-01294 trihydrochloride 通过与底物赖氨酸残基 N 端的氨基酸竞争结合来抑制 G9a/GLP。BIX-01294 trihydrochloride 是一种 (1H-1,4-diazepin-1-yl)-quinazolin-4-yl 胺衍生物，可诱导坏死性凋亡 (necroptosis) 和自噬。BIX-01294 trihydrochloride 在复发性肿瘤细胞中具有抗肿瘤活性。

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BIX-01294 trihydrochloride

BIX-01294 trihydrochloride Chemical Structure

CAS No. : 1392399-03-9

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规格 价格 是否有货 数量
5 mg ￥720
In-stock
10 mg ￥1153
In-stock
25 mg ￥2400
In-stock
50 mg ￥3100
In-stock
100 mg ￥4650
In-stock
200 mg   询价  
500 mg   询价  

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Customer Review

Other Forms of BIX-01294 trihydrochloride:

BIX-01294 trihydrochloride 相关抗体

Top Publications Citing Use of Products

    BIX-01294 trihydrochloride purchased from MCE. 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 MCE. 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

    查看 Histone Methyltransferase 亚型特异性产品:

    查看所有亚型
    EZH1 EZH2 DOT1L SMYD2 SMYD3 SUV39H2/KMT1B EHMT2/G9a/KMT1C EHMT1/GLP/KMT1D ASH1L/KMT2H SETDB1/KMT2G SETD2/KMT3A NSD2/MMSET/WHSC1 SETD7/KMT7 SETD8/KMT5A PRMT1 PRMT3 PRMT4 PRMT5 PRMT6 PRMT7 PRMT8

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    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]
    体外研究
    (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.

    BIX-01294 trihydrochloride 相关抗体:

    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.
    体内研究
    (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.
    分子量

    600.02

    Formula

    C28H41Cl3N6O2
    CAS 号
    性状

    固体

    颜色

    Light yellow to yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    溶解性数据
    细胞实验： 

    H2O 中的溶解度 : ≥ 100 mg/mL (166.66 mM)

    DMSO 中的溶解度 : 58.33 mg/mL (97.21 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    * "≥" means soluble, but saturation unknown.

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 1.6666 mL 8.3331 mL 16.6661 mL
    5 mM 0.3333 mL 1.6666 mL 3.3332 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    计算结果
    工作液所需浓度 : mg/mL
    该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
    您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
    纯度 & 产品资料
    参考文献

    BIX-01294 trihydrochloride 相关分类

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
    储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO / H2O 1 mM 1.6666 mL 8.3331 mL 16.6661 mL 41.6653 mL
    5 mM 0.3333 mL 1.6666 mL 3.3332 mL 8.3331 mL
    10 mM 0.1667 mL 0.8333 mL 1.6666 mL 4.1665 mL
    15 mM 0.1111 mL 0.5555 mL 1.1111 mL 2.7777 mL
    20 mM 0.0833 mL 0.4167 mL 0.8333 mL 2.0833 mL
    25 mM 0.0667 mL 0.3333 mL 0.6666 mL 1.6666 mL
    30 mM 0.0556 mL 0.2778 mL 0.5555 mL 1.3888 mL
    40 mM 0.0417 mL 0.2083 mL 0.4167 mL 1.0416 mL
    50 mM 0.0333 mL 0.1667 mL 0.3333 mL 0.8333 mL
    60 mM 0.0278 mL 0.1389 mL 0.2778 mL 0.6944 mL
    80 mM 0.0208 mL 0.1042 mL 0.2083 mL 0.5208 mL
    H2O 100 mM 0.0167 mL 0.0833 mL 0.1667 mL 0.4167 mL

    * 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

    Help & FAQs
    • 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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