1. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation Apoptosis Cytoskeleton Cell Cycle/DNA Damage
  2. Pyruvate Kinase Reactive Oxygen Species (ROS) Apoptosis Microtubule/Tubulin
  3. PKM2-IN-11

PKM2-IN-11 是一种 PKM2 抑制剂 (IC50 = 0.363 μM)。PKM2-IN-11 具有双重作用机制,包括抑制丙酮酸激酶 M2 (PKM2) 和稳定微管。PKM2-IN-11 能降低 MCF-7 细胞中 PKM2 蛋白的水平。PKM2-IN-11 可略微降低活性氧 (ROS) 水平,并显著增加早期凋亡 (apoptosis) 细胞。PKM2-IN-11 可诱导 G2/M 期阻滞。PKM2-IN-11 可用于乳腺癌的研究。

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PKM2-IN-11

PKM2-IN-11 Chemical Structure

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PKM2-IN-11 is a PKM2 inhibitor (IC50 = 0.363 μM). PKM2-IN-11 has dual mechanisms involving pyruvate kinase M2 (PKM2) inhibition and microtubule stabilization. PKM2-IN-11 can decrease PKM2 protein levels in MCF-7 cells. PKM2-IN-11 can slightly reduce reactive oxygen species (ROS) levels and significantly increase early apoptotic cells. PKM2-IN-11 induces G2/M phase arrest. PKM2-IN-11 can be used for the study of breast cancer[1].

IC50 & Target

PKM2

0.363 μM (IC50)

体外研究
(In Vitro)

PKM2-IN-11 (Compound 30o) (1-25 μM,24 小时) 对 MCF-7 细胞表现出强效的抗增殖活性 (IC50 = 10.2 μM),且对 HEK-293 细胞无细胞毒性作用[1]
PKM2-IN-11 (1-5 μM) 可剂量依赖性地降低 MCF-7 细胞中 PKM2 蛋白的表达水平[1]
PKM2-IN-11 (5 μM) 可提高微管聚合速率 (Vmax) 并稳定微管生长[1]
PKM2-IN-11 可轻微降低 MCF-7 细胞中活性氧 (ROS) 水平并诱导线粒体膜电位 (ΔΨm) 去极化,从而导致红/绿荧光比值降低[1]
PKM2-IN-11 (5 μM) 可显著增加 MCF-7 细胞中早期凋亡细胞,晚期凋亡细胞比例较低,并导致 G2/M 期阻滞 (23%)[1]

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

Cell Proliferation Assay[1]

Cell Line: MCF-7 cells
Concentration: 1 μM, 5 μM, 10 μM, 25 μM
Incubation Time: 24 h
Result: Exhibited potent antiproliferative activity (IC50 = 10.2 ± 0.07 μM) against MCF-7 cells.
分子量

462.28

Formula

C21H19IO4

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 *
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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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PKM2-IN-11
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HY-178441
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