2. Metabolic Enzyme/Protease NF-κB Immunology/Inflammation
  3. Glutaminase Reactive Oxygen Species (ROS)
  4. Glutaminase C-IN-3

Glutaminase C-IN-3 是一种强效的谷氨酰胺酶 C (GAC) 变构抑制剂，EC50 值为 116 nM。Glutaminase C-IN-3 通过阻断谷氨酰胺代谢来调节细胞代谢物并增加活性氧 (ROS) 的产生。在 A549 异种移植小鼠模型中，Glutaminase C-IN-3 表现出显著的抗肿瘤活性。Glutaminase C-IN-3 可用于非小细胞肺癌 (NSCLC) 的研究。

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Glutaminase C-IN-3

Glutaminase C-IN-3 Chemical Structure

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Glutaminase C-IN-3 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

Glutaminase C-IN-3 is a potent allosteric inhibitor of Glutaminase C (GAC) with an EC50 of 116 nM. Glutaminase C-IN-3 regulates cellular metabolites and increases reactive oxygen species (ROS) production by blocking glutamine metabolism. Glutaminase C-IN-3 exhibits strong antitumor activity in an A549 xenograft mouse model. Glutaminase C-IN-3 can be used for the research of non-small cell lung cancer (NSCLC)[1].

IC50 & Target[1]

GAC

116 nM (EC50)

体外研究
(In Vitro)

Glutaminase C-IN-3 (compound 16) (72 小时) 在 A549 细胞中表现出强大的抗增殖活性 (IC50 = 2.45 nM)，同时对正常细胞 (BEAS-2B) 表现出选择性，IC50 为 1.12 µM[1]。
Glutaminase C-IN-3 (30-300 nM，16 小时) 显著破坏谷氨酰胺代谢，导致 A549 细胞中谷氨酸/谷氨酰胺比率浓度依赖性降低[1]。
Glutaminase C-IN-3 (300 nM-1 µM，16 小时) 可诱导 A549 细胞中 ROS 水平呈剂量依赖性增加，表明 ROS 生成增强和氧化还原稳态丧失[1]。
Glutaminase C-IN-3 (5 μM，1 小时) 在模拟胃液 (SGF) 和模拟肠液 (SIF) 中表现出较高的稳定性[1]。
Glutaminase C-IN-3 (5 μM，0.25-2 小时) 在大鼠肝微粒体中表现出中等代谢稳定性[1]。

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

Glutaminase C-IN-3 相关抗体:
体内研究
(In Vivo)

Glutaminase C-IN-3 (compound 16) (10 和 30 mg/kg，腹腔注射，每日一次，持续 22 天) 在 A549 异种移植小鼠模型中表现出抗肿瘤功效，且安全性良好[1]。

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

Animal Model: Male Balb/c nude mice inoculated with A549 tumor fragments[1]
Dosage: 10 and 30 mg/kg
Administration: i.p., once daily for 22 days
Result: Showed tumor growth inhibition with a TGI of 25.8% at 10 mg/kg.
Did not significantly enhance efficacy at 30 mg/kg.
Showed no significant body weight decrease.
分子量

656.68

Formula

C31H31F3N6O5S
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

Glutaminase C-IN-3 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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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)
× = ×
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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:

Glutaminase C-IN-3GlutaminaseReactive Oxygen Species (ROS)AntitumorAllosteric inhibitorProdrugGACInhibitorinhibitorinhibit

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