2. PI3K/Akt/mTOR Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage
  3. MELK PDGFR Haspin Kinase
  4. MELK-8a

MELK-8a  (Synonyms: NVS-MELK8a)

目录号: HY-100368 纯度: 98.32%
COA 产品使用指南

摩尔计算器

MELK-8a (NVS-MELK8a) 是一种高效的选择性母体胚胎亮氨酸拉链激酶 (MELK) 抑制剂，IC50 为 2 nM。MELK-8a 还抑制 Flt3 (ITD)、Haspin、PDGFRα，IC50 分别为 0.18、0.19 和 0.42 μM。 MELK 在调节癌细胞的细胞有丝分裂中发挥着重要作用。

在相同的摩尔浓度下，化合物盐形式与游离形式有相同的生物活性，但盐形式 MELK-8a hydrochloride 通常具有更好的水溶性和稳定性。

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MELK-8a Chemical Structure

MELK-8a Chemical Structure

CAS No. : 1922153-17-0

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规格 是否有货
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MELK-8a 的其他形式现货产品:

Customer Review

Other Forms of MELK-8a:

MELK-8a 相关抗体

Top Publications Citing Use of Products

    MELK-8a purchased from MCE. Usage Cited in: J Biol Chem. 2020 Feb 21;295(8):2359-2374.  [Abstract]

    Asynchronous MDA-MB-468 cells are treated with DMSO or 0.5, 1, or 3 μM 8a for 1, 6, or 24h. Cells are harvested and immunoblotted with the indicated antibodies.

    MELK-8a purchased from MCE. Usage Cited in: J Biol Chem. 2020 Feb 21;295(8):2359-2374.  [Abstract]

    Delayed mitotic entry caused by 8a is associated with delayed activation of Aurora A, Aurora B, and CDK1. HeLaS3 cells are synchronized at G1/S with double thymidine block and released into DMSO or 3 μM 8a. Cells are collected starting at 6h post-release, with subsequent collections completed every 0.5 or 1h, over a 12h timecourse. Cells are lysed and immunoblotted with the indicated antibodies. The split in the image indicates that the samples from DMSO and 3 μM 8a conditions are blotted sepa.

    MELK-8a purchased from MCE. Usage Cited in: J Biol Chem. 2020 Feb 21;295(8):2359-2374.  [Abstract]

    HeLaS3 cells treated with 8a complete mitosis and begin the subsequent cell cycle following delayed mitotic entry. HeLaS3 cells are synchronized at G1/S with double thymidine block and released into DMSO or 3 μM 8a. Cells are collected starting at 6h post-release, with subsequent collections completed every 2h over a 20h timecourse. Cells are lysed and immunoblotted with the indicated antibodies. The split in the image indicates that the samples from DMSO and 3 μM 8a conditions are blotted sepa

    MELK-8a purchased from MCE. Usage Cited in: J Biol Chem. 2020 Feb 21;295(8):2359-2374.  [Abstract]

    MELK inhibition with 3 μM 8a causes delayed mitotic entry. HeLaS3 cells are synchronized at G1/S with double thymidine block and released into DMSO, 1 μM, or 3 μM 8a. Cells are collected every 2h over a 12h timecourse. Cells are lysed and immunoblotted with the indicated antibodies. The splits in the image indicate that the samples from DMSO, 1 μM, and 3 μM 8a conditions are immunoblotted separately due to space constraints. Asynchronous HeLaS3 lysate is loaded in the lanes labeled “A” in order

    MELK-8a purchased from MCE. Usage Cited in: Cell Rep. 2017 Dec 5;21(10):2829-2841.  [Abstract]

    A375 cells are treated with MELK-8a for 48 h and analyzed for indicated proteins by immunoblot analysis. ACTINB is used for as a loading control.

    查看 PDGFR 亚型特异性产品:

    查看所有亚型
    PDGFR PDGFRβ PDGFRα

    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    MELK-8a (NVS-MELK8a) is a highly potent and selective maternal embryonic leucine zipper kinase (MELK) inhibitor with IC50 of 2 nM. MELK-8a also inhibits Flt3 (ITD), Haspin, PDGFRα with IC50s of 0.18, 0.19, and 0.42 μM, respectively. MELK plays an essential role in regulating cell mitosis in a subset of cancer cells[1].

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    MCF7 IC50
    3.68 μM
    Compound: 8a
    Antiproliferative activity against MELK-independent ER-positive human MCF7 cells assessed as reduction in cell viability after 7 days by CellTiter-Glo assay
    Antiproliferative activity against MELK-independent ER-positive human MCF7 cells assessed as reduction in cell viability after 7 days by CellTiter-Glo assay
    		[PMID: 27187609]
    MDA-MB-468 IC50
    0.11 μM
    Compound: 8a
    Antiproliferative activity against MELK-dependent human MDA-MB-468 cells assessed as reduction in cell viability after 7 days by CellTiter-Glo assay
    Antiproliferative activity against MELK-dependent human MDA-MB-468 cells assessed as reduction in cell viability after 7 days by CellTiter-Glo assay
    		[PMID: 27187609]
    分子量

    432.56

    Formula

    C25H32N6O
    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 6 months
    -20°C 1 month
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 10 mg/mL (23.12 mM; 超声助溶 (<60°C); 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 2.3118 mL 11.5591 mL 23.1182 mL
    5 mM 0.4624 mL 2.3118 mL 4.6236 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。-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。

    • 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
    纯度 & 产品资料
    参考文献

    MELK-8a 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。-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 1 mM 2.3118 mL 11.5591 mL 23.1182 mL 57.7955 mL
    5 mM 0.4624 mL 2.3118 mL 4.6236 mL 11.5591 mL
    10 mM 0.2312 mL 1.1559 mL 2.3118 mL 5.7795 mL
    15 mM 0.1541 mL 0.7706 mL 1.5412 mL 3.8530 mL
    20 mM 0.1156 mL 0.5780 mL 1.1559 mL 2.8898 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.

    Keywords:

    MELK-8a1922153-17-0NVS-MELK8aMELKPDGFRHaspin KinaseMaternal embryonic leucine zipper kinasePlatelet-derived growth factor receptormaternal embryonic leucine zipper kinaseMELK inhibitorcell mitosiscancer cellsInhibitorinhibitorinhibit

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    目录号：
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