2. PI3K/Akt/mTOR Metabolic Enzyme/Protease Immunology/Inflammation NF-κB Apoptosis
  3. PDK-1 Reactive Oxygen Species (ROS) Apoptosis Oxidative Phosphorylation
  4. PDK1-IN-5

PDK1-IN-5 是一种选择性 PDK1 抑制剂。PDK1-IN-5 通过抑制 PDK1 降低磷酸化水平从而激活 PDH。PDK1-IN-5 能有效逆转 Warburg 效应，通过增加乙酰辅酶 A、减少乳酸、升高线粒体 ROS 并随后诱导细胞凋亡 (apoptosis)，将细胞能量代谢从糖酵解 (oxidative phosphorylation) 转向氧化磷酸化。PDK1-IN-5 在体内能强效抑制肿瘤生长且不引起系统性毒性。PDK1-IN-5 可用于肺腺癌、人非小细胞肺腺癌以及胃癌和结直肠癌的研究。

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PDK1-IN-5

PDK1-IN-5 Chemical Structure

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PDK1-IN-5 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PDK1-IN-5 is a selective PDK1 inhibitor. PDK1-IN-5 activaties PDH by diminishing phosphorylation level via PDK1 inhibition. PDK1-IN-5 effectively reverses the Warburg effect and shifts cellular energy metabolism from glycolysis toward oxidative phosphorylation by increased acetyl-CoA, reduced lactate, elevated mitochondrial ROS, and subsequent induction of apoptosis. PDK1-IN-5 robustly inhibits tumor growth in vivo without inducing systemic toxicity. PDK1-IN-5 can be used for lung adenocarcinoma, human non-small cell lung adenocarcinoma and gastric colorectal[1].

体外研究
(In Vitro)

PDK1-IN-5 (compound D16) (48 h)，对 A549 (肺腺癌)、PC9 (肺腺癌)、H1975 (人非小细胞肺腺癌)、HGC-27 (胃癌) 和 HCT-116 (结直肠癌) 细胞表现出选择性和优异的抗增殖活性，其 IC50 值分别为 0.86、5.99、4.92、2.48 和 1.15 μM[1]。
PDK1-IN-5 表现出强烈的 PDK1 抑制活性，抑制率为 53.20%[1]。
PDK1-IN-5 (0-12 μM，0.5 小时) 在 A549 和 PC9 细胞中通过抑制 PDK1 活性来降低 PDH 的磷酸化水平，从而激活 PDH[1]。
PDK1-IN-5 (0.4-1.6 μM，14 天) 以浓度依赖的方式抑制 A549 和 PC9 细胞的增殖能力[1]。
PDK1-IN-5 (0.4-1.6 μM 及 3-12 μM，24 小时) 以剂量依赖的方式抑制 A549 和 PC9 细胞的迁移[1]。
PDK1-IN-5 (0.2-3.2 μM 及 1.5-24 μM，48 小时) 能提升线粒体 ROS 水平，并诱导浓度依赖性的细胞凋亡[1]。
PDK1-IN-5 (0.2-3.2 μM 及 1.5-24 μM，24 和 48 小时) 通过强效抑制 PDK1 来逆转 Warburg 效应，从而有效地改变肿瘤细胞代谢，将能量平衡从糖酵解转向氧化磷酸化，突显了其治疗潜力[1]。

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

PDK1-IN-5 相关抗体:

Western Blot Analysis[1]

Cell Line: A549 and PC9 cells
Concentration: 0, 0.4, 0.8 and 1.6 μM (A549); 0, 3, 6, 12 μM (PC9)
Incubation Time: 0.5 h
Result: Decreased the expression of phosphorylated protein pPDH (serine 293) in a concentration-dependent manner.
Reduced phosphorylation level and raised PDHA1 expression.

Cell Proliferation Assay[1]

Cell Line: A549 and PC9 cells
Concentration: 0, 0.4, 0.8 and 1.6 μM (A549); 0, 3, 6, 12 μM (PC9)
Incubation Time: 14 days
Result: Achieved 98 % inhibition of colony formation at 14 day in high concentration treatment (1.6 μM).

Cell Migration Assay [1]

Cell Line: A549 and PC9 cells
Concentration: 0, 0.4, 0.8 and 1.6 μM (A549); 0, 3, 6, 12 μM (PC9)
Incubation Time: 24 h
Result: Reached 80.5 % inhibition at the highest concentration.

Cell Cytotoxicity Assay[1]

Cell Line: A549 and PC9 cells
Concentration: 0.2, 0.8 and 3.2 μM (A549); 1.5, 6, 24 μM (PC9)
Incubation Time: 48 h
Result: Induced PC9 cells apoptotic rate at 1.5, 6, and 24 μM with 7.0%, 12.5%, and 17.7%, respectively.
Induced A549 cells apoptotic rate at 0.2, 0.8, and 3.2 μM with 16.1%, 26.6%, and 30.7%, respectively.
体内研究
(In Vivo)

PDK1-IN-5 (compound D16) (5-20 mg/kg，腹腔注射，每 2 天一次，持续 14 天) 在 A549 和 PC9 移植瘤小鼠模型中，通过抑制肿瘤增殖发挥体内抗肿瘤作用[1]。

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

Animal Model: Male BALB/c-nu nude mice (4 weeks old) were implanted with A549 and PC9 cells[1].
Dosage: 5, 10, and 20 mg/kg
Administration: i.p., every 2 days for 14 days
Result: Revealed no pathological abnormalities in Hematoxylin-Eosin (H&E) in major organs (heart, liver, spleen, lung, kidney) from the 20 mg/kg.
Maintained stable body weights in animals throughout the experimental period.
Downregulated PDK1 expression and reduced the number of Ki-67-positive cells in treated tumors.
分子量

394.17

Formula

C16H12Cl2F3NO3
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

PDK1-IN-5 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

PDK1-IN-5PDK-1Reactive Oxygen Species (ROS)ApoptosisOxidative Phosphorylation3-Phosphoinositide-dependent protein kinase 1PDK1PDHWarburg effectacetyl-CoAROSapoptosislung adenocarcinomahuman non-small cell lung adenocarcinoma and gastric colorectal.Inhibitorinhibitorinhibit

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