1. Cell Cycle/DNA Damage PI3K/Akt/mTOR Apoptosis
  2. DNA-PK Apoptosis
  3. NU 7026

NU 7026  (Synonyms: LY293646)

目录号: HY-15719 纯度: 99.86%
COA 产品使用指南

NU 7026 (LY293646) 是一种新型特异性的 DNA-PK 抑制剂,IC50 为 0.23 μM,也抑制 PI3KIC50 为 13 μM。

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NU 7026 Chemical Structure

NU 7026 Chemical Structure

CAS No. : 154447-35-5

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规格 价格 是否有货 数量
5 mg ¥519
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10 mg ¥760
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25 mg ¥1710
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50 mg ¥2907
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100 mg ¥4070
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500 mg   询价  

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Top Publications Citing Use of Products

    NU 7026 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2019 May;76(10):2015-2030.  [Abstract]

    Western blots of NONO and SFPQ in MDA-MB-468 cell lysates immunoprecipitated with IGFBP-3-Fab beads, showing that incubation overnight with 20 μM NU7026 block the formation of IGFBP-3 complexes with NONO and SFPQ formed in response to 20 μM etopside.

    NU 7026 purchased from MCE. Usage Cited in: Cell Mol Life Sci. 2019 May;76(10):2015-2030.  [Abstract]

    Western blots of NONO and SFPQ in MDA-MB-468 cell lysates immunoprecipitated with IGFBP-3-Fab beads, showing that incubation overnight with 20 μM NU7026 block the formation of IGFBP-3 complexes with NONO and SFPQ formed in response to 20 μM etopside.
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    NU 7026 (LY293646) is a novel specific DNA-PK inhibitor with IC50 of 0.23 μM, also inhibits PI3K with IC50 of 13 μM.

    IC50 & Target[1]

    DNA-PK

    0.23 μM (IC50)

    PI3K

    13 μM (IC50)

    体外研究
    (In Vitro)

    NU7026 (10 μM) potentiates ionizing radiation (IR) cytotoxicity [potentiation factor at 90% cell kill (PF90)=1.51±0.04] in exponentially growing DNA-PK proficient but not deficient cells[1]. NU7026 synergistically sensitizes I83 cells to Chlorambucil (CLB) 3.5-fold[2].NU7026, a novel inhibitor of the DNA repair enzyme DNA-dependent protein kinase (DNA-PK). At a dose of 10 μM, which is nontoxic to cells per se, a minimum NU7026 exposure of 4 h in combination with 3 Gy radiation is required for a significant radiosensitisation effect in CH1 human ovarian cancer cells[3].
    ? Solution in vitro: NU7026 is dissolved in anhydrous DMSO. NU7026 is added to cells to a final concentration of 0.25% DMSO (v/v)[4].

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

    体内研究
    (In Vivo)

    NU7026, a novel inhibitor of the DNA repair enzyme DNA-dependent protein kinase (DNA-PK). Following intravenous administration to mice at 5 mg/kg, NU7026 underwent rapid plasma clearance (0.108 L/h) and this is largely attributed to extensive metabolism. Bioavailability following interperitoneal (i.p.) and p.o. administration at 20 mg/kg is 20 and 15%, respectively[3].
    ? Solution in vivo:
    ? NU7026 is formulated in 10% DMSO and 5% Tween 20 in saline (i.p. and p.o.) (Mice)[3].
    ? NU7026 is formulated in 10% ethanol, 25% PEG 200 and 5% Tween 20 in saline (i.v.)[3].

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

    分子量

    281.31

    Formula

    C17H15NO3

    CAS 号
    性状

    固体

    颜色

    Off-white to light yellow

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    溶解性数据
    In Vitro: 

    DMSO 中的溶解度 : 2.5 mg/mL (8.89 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)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 3.5548 mL 17.7740 mL 35.5480 mL
    5 mM 0.7110 mL 3.5548 mL 7.1096 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, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6个月内使用。

    • 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

    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
    纯度 & 产品资料

    纯度: 99.86%

    参考文献
    Kinase Assay
    [1]

    Mammalian DNA-PK (500 ng/μL) is isolated from HeLa cell nuclear extract after chromatography using Q-Sepharose, S-Sepharose, and Heparin agarose. DNA-PK (250 ng) activity is measured at 30°C, in a final volume of 40 μL, in buffer containing 25 mM HEPES (pH 7.4), 12.5 mM MgCl2, 50 mM KCl, 1 mM DTT, 10% v/v Glycerol, 0.1% w/v NP-40, and 1 mg of the substrate GST-p53N66 (the NH2-terminal 66 amino acid residues of human wild-type p53 fused to glutathione S-transferase) in polypropylene 96-well plates. To the assay mix, varying concentrations of inhibitor (in DMSO at a final concentration of 1% v/v) are added. After 10 min of incubation, ATP is added to give a final concentration of 50 μM, along with a 30-mer double-stranded DNA oligonucleotide (final concentration of 0.5 ng/mL), to initiate the reaction. After 1 h with shaking, 150 μL of PBS are added to the reaction, and 5 μL are then transferred to a 96-well opaque white plate containing 45 μL of PBS per well, where the GSTp53N66 substrate is allowed to bind to the wells for 1 h. To detect the phosphorylation event on the serine 15 residue of p53 elicited by DNA-PK, a p53 phosphoserine-15 antibody is used in a basic ELISA procedure. An antirabbit horseradish peroxidase-conjugated secondary antibody is then used in the ELISA before the addition of chemiluminescence reagent to detect the signal as measured by chemiluminescent counting via a TopCount NXT[1].

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

    Cell Assay
    [2]

    I83 cells are plated in RPMI 1640 medium with 10% FBS (1.5×105 cells/mL) and treated with vehicle (DMSO), 5 μM CLB, CLB IC50, 10 μM NU7026, or the combination of both drugs for 0, 6, 24, and 48 h. Cell cycle distribution, apoptosis, DNA-PK phosphorylation, and γH2AX determination are determined, and they are expressed as a percentage of cells in each phase of the cycle. DNA content is analyzed with a FACSCalibur flow cytometer equipped with CellQuest software[2].

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

    Animal Administration
    [3]

    Mice[3]
    Female BALB/c mice are used. NU7026 is formulated in 10% DMSO and 5% Tween 20 in saline for i.p. and perorally (p.o.) administration at 20 and 50 mg/kg, respectively. For i.v. dosing at 5 mg/kg, NU7026 is formulated in 10% ethanol, 25% PEG 200 and 5% Tween 20 in saline. Control animals receive the vehicle alone. Groups of three mice are injected per time point. Blood is collected by cardiac puncture following transient anaesthesia with halothane at 0.083, 0.25, 0.5, 1, 2, 4, 6, and 24 h post administration. Following centrifugation at 1500 g for 2 min to obtain plasma, samples are stored at −20°C until analysis. For urinary excretion studies, NU7026 is administered at 5 mg/kg i.v. Urine is collected over 24 h in metabolic cages, and stored at −20°C until required.

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

    参考文献

    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, 1 years; -20°C, 6 months。-80°C储存时,请在1年内使用, -20°C储存时,请在6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 1 mM 3.5548 mL 17.7740 mL 35.5480 mL 88.8699 mL
    5 mM 0.7110 mL 3.5548 mL 7.1096 mL 17.7740 mL
    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.

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