1. Apoptosis
  2. Apoptosis Bcl-2 Family MDM-2/p53
  3. Lobetyol

Lobetyol 是一种天然化合物,可从 Lobelia chinensis 中分离得到。 Lobetyol 在 MKN45 细胞中诱导细胞凋亡 (apoptosis) 和细胞周期停滞。 Lobetyol 具有抗病毒、抗炎和抗肿瘤活性。

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Lobetyol Chemical Structure

Lobetyol Chemical Structure

CAS No. : 136171-87-4

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查看 Bcl-2 Family 亚型特异性产品:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Lobetyol is a natural compound that can be isolated from Lobelia chinensis. Lobetyol induces apoptosis and cell cycle arrest in MKN45 cells. Lobetyol shows anti-virus, anti-inflammation and anti-tumor activity[1][2]. Lobetyol is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.

IC50 & Target

Bax

 

Bcl-2

 

体外研究
(In Vitro)

Lobetyol (0-100 μg/mL, 0-48 h) 在 MKN45 细胞中导致剂量和时间依赖性增殖抑制[1]
Lobetyol (0-100 μg/mL, 48 h) 以时间和剂量依赖的方式诱导 MKN45 细胞细胞凋亡和细胞周期停滞[1]
Lobetyol (0-100 μg/mL, 48 h) 增加 Bax、P53 的表达水平,降低 Bcl-2 的表达水平[1]

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

Cell Proliferation Assay[1]

Cell Line: MKN45 cells
Concentration: 0 μg/mL, 50 μg/mL, 75 μg/mL, 100 μg/mL
Incubation Time: 12 h, 24 h, 48 h
Result: Showed a dose-and time-dependent proliferation inhibition in MKN45 cells, with an IC50 of 71.47 ± 4.29 μg/mL at 48 h. Exhibited more safety on L02 and HEK293 human normal cell lines.

Apoptosis Analysis[1]

Cell Line: MKN45 cells
Concentration: 0 μg/mL, 50 μg/mL, 75 μg/mL, 100 μg/mL
Incubation Time: 48 h
Result: Increased the apoptotic population in MKN45 cells in a dose-dependent manner. Flow cytometic assay of Annexin-V/PI revealed apoptotic populations under increasing dose of lobetyol ranging from 0 μg/mL, 50 μg/mL, 75 μg/mL, to 100 μg/mL are 5.5%, 13.74%, 27.32% to 31.57%, respectively.

Western Blot Analysis[1]

Cell Line: MKN45 cells
Concentration: 0 μg/mL, 50 μg/mL, 75 μg/mL, 100 μg/mL
Incubation Time: 12 h, 24 h, 48 h
Result: Increased the expression level of Bax, P53, and decreased the expression level of Bcl-2. The release of cytochrome c was detected, followed by caspase-9 and -3 activations.
体内研究
(In Vivo)

Lobetyol (0-10 mg/kg,每3天一次)抑制 MKN45 裸鼠模型中的肿瘤生长[1]

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

Animal Model: BALB/C nude mice (6 weeks-old, injected intraperitoneally with MKN45 cells)[1]
Dosage: 0, 2, 5, 10 mg/kg
Administration: Once per 3 days
Result: Suppressed tumor growth in MKN45 nude models. The protein levels of Ki67 in MKN45 cells were significantly decreased. Meanwhile, cleaved-caspase-3 positive MKN45 cells were found increased with the tendency of lobetyol concentrations in the study in vivo.
分子量

234.29

Formula

C14H18O3

CAS 号
结构分类
初始来源
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

Lobetyol 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.

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Lobetyol
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