2. Metabolic Enzyme/Protease Apoptosis Immunology/Inflammation NF-κB
  3. Pyruvate Kinase Apoptosis Reactive Oxygen Species (ROS) Caspase
  4. PKM2-IN-13

PKM2-IN-13 是一种选择性的 PKM2 抑制剂对 PKM2 的 IC50 值为 55.13 μM。PKM2-IN-13 表现出广谱的抗癌活性，对正常细胞具有低毒性。PKM2-IN-13 通过提高活性氧 (ROS) 水平和激活 Caspase-3/7 来诱导细胞凋亡 (apoptosis)，并在体外与丙酮酸激酶 M2 相互作用，抑制其糖酵解活性。PKM2-IN-13 安全性良好，体内实验未观察到显著不良反应。PKM2-IN-13 可用于口腔鳞状细胞癌，结肠癌，乳腺癌和黑色素瘤的研究。

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PKM2-IN-13

PKM2-IN-13 Chemical Structure

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PKM2-IN-13 相关抗体

Top Publications Citing Use of Products

查看 Caspase 亚型特异性产品:

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

PKM2-IN-13 is a selective PKM2 inhibitor inhibiting PKM2 with an IC50 value of 55.13 μM. PKM2-IN-13 exhibits broad-spectrum anticancer activity with low toxicity to normal cells. PKM2-IN-13 induces apoptosis by elevated ROS levels and activation of caspases 3/7, and interacts with and inhibits the glycolytic activity of Pyruvate Kinase M2 in virto. PKM2-IN-13 demonstrates a favorable safety profile with no significant adverse effects in vivo. PKM2-IN-13 can be used for oral squamous cell carcinoma (OSCC), colon carcinoma, breast cancer and melanoma research[1].

IC50 & Target[1]

PKM2

55.13 μM (IC50)

Caspase 3

 

Caspase-7

 

体外研究
(In Vitro)

PKM2-IN-13 (compound 7f) ( 48 小时)，在 SCC-9 细胞中诱导约 5% 的溶血水平，并有效诱导细胞毒性(IC50 = 12.29 μM)，对多种癌细胞系具有选择性抑制活性，包括口腔鳞癌细胞 SCC-9 (IC50 = 12.29 μM；SI = 1.85)、SCC-4 (IC50 = 7.93 μM)、SCC-25 (IC50 = 11.09 μM)，原代牙龈成纤维细胞 (IC50 = 22.77 μM)，以及其他癌细胞系 4T1 (IC50 = 7.63 μM)、Hep-G2 (IC50 = 15.98 μM)、HCT116 (IC50 = 6.72 μM)、B16−F10 (IC50 = 4.93 μM)[1]。
PKM2-IN-13 (24.58 μM，0-48 小时) 在 SCC-9 细胞中表现出显著的增殖抑制能力，在处理 6 小时后即可观察到细胞间连接破坏、细胞膜起泡及随之而来的增殖停滞，且在 12 小时后这些效应更为明显[1]。
PKM2-IN-13 (24.58 μM，24 和 48 小时) 在 SCC-9 细胞中于 24 小时诱导 S 期阻滞，随后在 12-24 小时内通过触发内在的 Caspase 依赖性凋亡通路 (而非坏死性凋亡) 导致癌细胞死亡[1]。
PKM2-IN-13 (24.58 μM，12-48 h) 在处理 12 和 24 小时后引起活性氧水平显著升高[1]。
PKM2-IN-13 (24.58 μM, 48 小时) 诱导的细胞毒性可经抗氧化剂 Antioxidant N-acetyl-L-cysteine (NAC) (10 mM) (HY-B0215) 预处理 2 小时得到保护，提示其作用机制与氧化应激相关[1][1]。

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

PKM2-IN-13 相关抗体:

Apoptosis Analysis[1]

Cell Line: SCC-9 cells
Concentration: 24.58 μM
Incubation Time: 12 h, 24 h
Result: Exhibited 2-fold high caspases 3 and 7 activity.

Cell Viability Assay[1]

Cell Line: SCC-9 cells
Concentration: 24.58 μM
Incubation Time: 24 h
Result: Significantly attenuated Cell death when pretreated with ZVAD (HY-164388) (20 μM).
Increased cell viability when pretreated with ZVAD.
Failed to reverse the cytotoxic effect when pretreatment with Nec-1 (HY-15760), either alone or in combination with ZVAD.
体内研究
(In Vivo)

PKM2-IN-13 (100-400 mg/kg，腹腔注射，14 天) 在 C57BL/6 小鼠中表现良好的安全性和较低的毒性[1]。

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

Animal Model: C57BL/6 mice (12 weeks old)[1]
Dosage: 100, 200, and 400 mg/kg
Administration: i.p., 14 days
Result: Detected no signs of morbidity or mortality.
Observed no significant changes in body weight or food intake throughout the study duration.
分子量

457.43

Formula

C25H19N3O6
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-IN-13 相关分类

  • 摩尔计算器

  • 稀释计算器

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

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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:

PKM2-IN-13Pyruvate KinaseApoptosisReactive Oxygen Species (ROS)CaspaseGlycolyticPyruvate Kinase M2Oral Squamous Cell CarcinomaPKM2apoptosisInhibitorinhibitorinhibit

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