1. Autophagy Apoptosis
  2. Autophagy Apoptosis
  3. Autophagy-IN-1

Autophagy-IN-1 是一种有效的细胞自噬 (autophagy) /线粒体自噬 (mitophagy) 抑制剂,通过在阻断癌细胞内自噬体-溶酶体融合的同时选择性地增加自噬通量来发挥作用。Autophagy-IN-1 可诱导细胞凋亡 (apoptosis) 和细胞周期阻滞。Autophagy-IN-1 在 HCT116 小鼠异种移植瘤模型中显著抑制肿瘤生长,且毒性低。Autophagy-IN-1 可用于结直肠癌的研究。

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Autophagy-IN-1 Chemical Structure

Autophagy-IN-1 Chemical Structure

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Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Autophagy-IN-1 is a potent autophagy/mitophagy inhibitor, acts by selectively increasing the autophagic flux while blocking the autophagosome-lysosome fusion in cancer cells. Autophagy-IN-1 can induce apoptosis and cell cycle arrest. Autophagy-IN-1 significantly inhibits tumor growth in an HCT116 xenograft mouse model and with low toxicity. Autophagy-IN-1 can be used for researching colorectal cancer[1].

IC50 & Target

Autophagy, Apoptosis[1]

体外研究
(In Vitro)

Autophagy-IN-1 (compound 6) (1 and 5 μM; 8 h) induces apoptosis of HCT116 cells concentration-dependently[1].
Autophagy-IN-1 (0.5, 1, 5 and 10 μM; 6 h) decreases pro-PARP1, pro-caspase 8 and pro-caspase 3; increases Cleaved-PARP1, Cleaved-caspase 8 and Cleaved-caspase 3 concentration-dependently[1].
Autophagy-IN-1 increases LC3B-II, p62, and LAMP1 in HCT116 and SW620 cells, and increases number of autophagic/mitophagic vacuoles in HCT116 cells[1].

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

Apoptosis Analysis[1]

Cell Line: HCT116 cells
Concentration: 1 and 5 μM
Incubation Time: 8 h
Result: Induced 10.11% and 33.52% apoptosis of HCT116 cells at 1 μM and 5 μM.

Western Blot Analysis[1]

Cell Line: HCT116 cells
Concentration: 0.5, 1, 5 and 10 μM
Incubation Time: 24 h
Result: Decreased pro-PARP1, pro-caspase 8 and pro-caspase 3; increased Cleaved-PARP1, Cleaved-caspase 8 and Cleaved-caspase 3 concentration-dependently.

Cell Autophagy Assay[1]

Cell Line: HCT116, SW620, and NCM460 cells
Concentration: 0.5, 1, 5 and 10 μM
Incubation Time: 0, 1, 2, 4, 9, 12 and 24 h
Result: Led to a time- and dose-dependent increase of the levels of LC3B-II, p62, and LAMP1 in HCT116 and SW620 cells, and increased number of autophagic/mitophagic vacuoles in HCT116 cells.
体内研究
(In Vivo)

Autophagy-IN-1 (50 and 100 mg/kg; IP, daily for 15 days) significantly inhibits tumor growth in an HCT116 xenograft mouse model[1].

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

Animal Model: Male BALB/c nude mice[1]
Dosage: 50 and 100 mg/kg
Administration: IP, daily for 15 days
Result: Significantly inhibited tumor growth and did not observe weight loss.
分子量

427.45

Formula

C23H25NO7

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

Autophagy-IN-1 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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