1. Metabolic Enzyme/Protease Membrane Transporter/Ion Channel Immunology/Inflammation NF-κB
  2. Creatine Kinase ATP Synthase Mitochondrial Metabolism Reactive Oxygen Species (ROS)
  3. GO847

GO847 是一种具有口服活性的酪蛋白激酶 2 (CK2) 抑制剂,其 IC50 为 40.2 nM。GO847 提高细胞内的 ATP 水平,损害线粒体代谢 (Mitochondrial metabolic) 灵活性,并促进线粒体过量产生 ROS。GO847 改变细胞昼夜节律的周期长度。GO847 抑制急性髓系白血病细胞生长。GO847 可用于急性髓系白血病的研究。

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GO847

GO847 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GO847 is an orally active casein kinase 2 (CK2) inhibitor with an IC50 of 40.2 nM. GO847 increases intracellular ATP levels, impairs Mitochondrial metabolic flexibility, and promotes excessive mitochondrial ROS production. GO847 alters the period length of cellular circadian rhythms. GO847 inhibits the growth of acute myeloid leukemia cells. GO847 can be used for the research of acute myeloid leukemia[1].

IC50 & Target[1]

CK2

40.2 nM (IC50)

体外研究
(In Vitro)

GO847 (1×10-11-1×10-6 M) 可在体外强效抑制 CK2 的酶活性,其 IC50 为 40.2 nM[1]
GO847 (0-20 μM; 48 h) 可呈剂量依赖性抑制小鼠急性髓系白血病 C1498 细胞 (IC50 = 5.1 μM) 和急性髓系白血病 THP-1 细胞 (IC50 = 1.7 μM) 的生长[1]
GO847 (0.9-8 μM; 24 h) 以剂量依赖方式抑制小鼠 AML C1498 细胞和 AML THP-1 细胞的细胞内 CK2 活性,处理 24 小时后可降低包括 AKT1 (S129) 在内的 CK2 底物的磷酸化水平[1]
GO847 (5 μM; 24 h) 处理小鼠 AML C1498 细胞 24 小时后,会损伤其线粒体代谢灵活性,降低备用呼吸容量,并消除线粒体抑制诱导的糖酵解代偿作用[1]
GO847 可提高小鼠 AML C1498 细胞内的 ATP 水平,升高线粒体膜电位,并促进线粒体过量产生 ROS[1]

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

Cell Proliferation Assay[1]

Cell Line: mouse AML C1498 cells, human AML THP-1 cells
Concentration: 0-20 μM
Incubation Time: 48 h
Result: Inhibited proliferation of both cell lines in a dose-dependent manner, with an IC50 of 5.1 μM for C1498 cells and 1.7 μM for THP-1 cells.

Western Blot Analysis[1]

Cell Line: mouse AML C1498 cells, human AML THP-1 cells
Concentration: 0.9-8 μM
Incubation Time: 24 h
Result: Caused a dose-dependent reduction in phosphorylation signals of CK2 substrates, including AKT1 (S129), in both C1498 and THP-1 cells.
Showed slightly less potent activity compared to GO289.
药代动力学
(Parmacokinetics)
Species Dose Route Cmax AUC0-t T1/2
Mice[1] 100 mg/kg i.p. 0.5 μM 4.0 μM·h 7.4 h
分子量

461.96

Formula

C21H24ClN5O3S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2
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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GO847
目录号:
HY-183265
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