2. Metabolic Enzyme/Protease PI3K/Akt/mTOR Protein Tyrosine Kinase/RTK JAK/STAT Signaling Apoptosis
  3. Pyruvate Kinase PDK-1 Akt EGFR Apoptosis
  4. PKM2/PDK1-IN-1

PKM2/PDK1-IN-1 是一种紫草素硫醚衍生物，是 PKM2/PDK1 的双重抑制剂。 PKM2/PDK1-IN-1抑制NSCLC细胞的增殖，并诱导细胞凋亡 (apoptosis)。 PKM2/PDK1-IN-1 诱导细胞间 ROS 产生，调节凋亡蛋白，参与线粒体和死亡受体通路。

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PKM2/PDK1-IN-1 Chemical Structure

PKM2/PDK1-IN-1 Chemical Structure

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PKM2/PDK1-IN-1 相关抗体

Top Publications Citing Use of Products

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Akt Akt1 Akt2 Akt3

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PKM2/PDK1-IN-1, one of shikonin thioether derivatives, is a dual inhibitor of PKM2/PDK1. PKM2/PDK1-IN-1 inhibits the proliferation of NSCLC cells, and induces apoptosis. PKM2/PDK1-IN-1 induces intercellular ROS production, and regulates the apoptotic proteins, to involves in mitochondrial and death receptor pathway[1].

IC50 & Target

PKM2, PDK-1[1]
体外研究
(In Vitro)

PKM2/PDK1-IN-1 (compound E5) (0.5-4 μM; 24 h) 显示出与 Gefitinib (HY-50895) 的协同抗癌作用[1]。
PKM2/PDK1-IN-1 (0.5 μM; 24 h) 调节线粒体和死亡受体通路的凋亡蛋白[1]。
PKM2/PDK1-IN-1 (0.5 μM, 1 μM; 24 h) 在肺癌细胞中引起线粒体跨膜电位 (ΔΨm) 耗散和细胞内 ROS 积累[1]。
PKM2/PDK1-IN-1 (1 μM，2 μM；24 小时) 抑制 PDK1 并增强 H1975 细胞中的下游 PDH 活性[1]。
PKM2/PDK1-IN-1 抑制细胞内 NADPH 浓度并增加 H1975 细胞的 ATP 产生[1]。

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

PKM2/PDK1-IN-1 相关抗体:

Cell Viability Assay[1]

Cell Line: H1975 cells
Concentration: 0.5 μM, 1 μM, 2 μM, 4 μM24 h; with 2.5-20 μM Gefitinib
Incubation Time: 24 h
Result: Synergistically induced cell apoptosis.

Western Blot Analysis[1]

Cell Line: H1975 cells
Concentration: 0.5 μM
Incubation Time: 24 h; with 10 μM Gefitinib
Result: Increased the protein levels of Cleaved Caspase-9, -3, and Cytochrome c. Deceased the protein levels of p-AKT, p-EGFR, Bcl-2.
体内研究
(In Vivo)

PKM2/PDK1-IN-1 (compound E5) (2.4 mg/kg，4.8 mg/kg；2天6次，共 11 天) 在体内抑制裸鼠H1975异种移植瘤的生长，毒副作用小[1]。

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

Animal Model: Nude mice with H1975 xenograft tumor (6-week-old)[1]
Dosage: 4.8 mg/kg; dispersed in 20% DMSO
Administration: IP; every two days for a total of 6 times, for 11 days
Result: Inhibited tumor growth.
Animal Model: For acute toxicity in ICR mice (8-week-old)[1]
Dosage: 2.4, 4.8, 9.6, 19.2, 38.4 mg/kg; dissolved in 20% DMSO
Administration: IP; singel dose; observed for 14 days
Result: Exhibited little side effect in mice.
分子量

697.92

Formula

C36H43NO7S3
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

PKM2/PDK1-IN-1 相关分类

  • 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.

Keywords:

PKM2/PDK1-IN-1Pyruvate KinasePDK-1AktEGFRApoptosis3-Phosphoinositide-dependent protein kinase 1PKBProtein kinase BEpidermal growth factor receptorErbB-1HER1Inhibitorinhibitorinhibit

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目录号：
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