1. Immunology/Inflammation NF-κB Metabolic Enzyme/Protease Apoptosis
  2. Reactive Oxygen Species (ROS) Apoptosis Mitochondrial Metabolism
  3. Mito-DHH chloride

Mito-DHH chloride 是一种线粒体靶向的儿茶酚型二苯基己三烯。Mito-DHH chloride 可快速在线粒体中积累,在碱性线粒体基质中发生自氧化以产生 ROS,通过双重抑制线粒体氧化磷酸化和糖酵解代谢触发 ROS 依赖性的 ATP 水平降低,并诱导癌细胞发生选择性凋亡 (apoptosis)。Mito-DHH chloride 可用于肺癌、肝癌、恶性黑色素瘤、结肠癌的相关研究。

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Mito-DHH chloride

Mito-DHH chloride Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Mito-DHH chloride is a mitochondria-targeted catechol-type diphenylhexatriene. Mito-DHH chloride rapidly accumulates in mitochondria and undergoes auto-oxidation in the alkaline mitochondrial matrix to generate ROS. Mito-DHH chloride triggers ROS-dependent reduction of ATP levels via dual inhibition of mitochondrial oxidative phosphorylation and glycolytic metabolism, and induces selective apoptosis in cancer cells. Mito-DHH chloride can be used in research related to lung cancer, liver cancer, malignant melanoma, and colon cancer[1].

体外研究
(In Vitro)

Mito-DHH (0.25-2.8 μM; 48 h) 可强效且选择性地杀伤 A549、HepG2、A375 和 SW620 癌细胞,而对正常 L02 细胞的杀伤作用较弱;其对 A549 细胞的活性最强,IC50 = 0.25 μM,选择性指数为 11.2[1]
Mito-DHH (0.25-0.5 μM; 10 days) 可在 0.25 μM 和 0.5 μM 浓度下损害 A549 细胞的长期克隆形成存活能力[1]
Mito-DHH (1 μM; 0.5-3 h) 可在 0.5 h 内快速且选择性地在 A549 细胞的线粒体中富集,而在 L02 细胞线粒体中的富集程度极低[1]
Mito-DHH (50 μM; 2 h) 在碱性条件 (pH 8 和 10) 下会促进自氧化以产生活性氧,且在更高 pH 下 ROS 的生成更为显著[1]
Mito-DHH (1 μM; 2 h) 在处理 2 h 后,相较于 L02 细胞,可优先在 A549 细胞中诱导线粒体超氧阴离子生成[1]
Mito-DHH (1 μM; 3 h) 处理 3 小时后,相较于 L02 细胞,会优先在 A549 细胞中诱导细胞内羟基自由基的产生[1]
Mito-DHH (1-2 μM; 6-12 h) 可在 6 h 和 12 h 后诱导 A549 细胞中依赖 ROS 的 ATP 生成减少,而在 10 μM 时对 L02 细胞的 ATP 水平无影响[1]
Mito-DHH (2 μM; 5 h) 可在处理 5 h 后抑制 A549 细胞的线粒体氧化磷酸化与细胞质糖酵解,从而诱导产生双效性能量危机[1]
Mito-DHH (1-2 μM; 18-24 h) 处理 18 h 和 24 h 后,可选择性破坏 A549 细胞的线粒体膜电位,而对 L02 细胞无影响[1]
Mito-DHH (10 μM; 1-12 h) 可诱导 A549 细胞发生晚期凋亡,其 PI 核定位从 6 h 开始可被检测到,并随时间推移逐渐发展[1]
Mito-DHH (1-2 μM; 48 h) 在处理 48 h 后,相较于 L02 细胞,可优先诱导 A549 细胞发生凋亡[1]
Mito-DHH (1-2 μM; 24 h) 处理 24 h 后,相较于 L02 细胞,可优先诱导 A549 细胞发生 G0/G1 期细胞周期阻滞[1]

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

Cell Proliferation Assay[1]

Cell Line: human lung cancer A549 cells
Concentration: 0.25 μM; 0.5 μM
Incubation Time: 10 days, with medium replacement every 48 h
Result: Significantly suppressed clonogenic survival, with colony counts of 83.5 (0.25 μM) and 61 (0.5 μM), compared to 138.8 in the control group.

Immunofluorescence[1]

Cell Line: human lung cancer A549 cells, normal human liver L02 cells
Concentration: 1 μM
Incubation Time: 0.5 h; 3 h
Result: Showed strong overlap with MitoTracker Deep Red in A549 cells, with a Pearson's colocalization coefficient of 0.91 at 0.5 h, indicating full mitochondrial localization within 30 min.
Displayed limited mitochondrial enrichment in L02 cells.

Apoptosis Analysis[1]

Cell Line: human lung cancer A549 cells
Concentration: 10 μM
Incubation Time: 1 h, 6 h, 9 h, 12 h
Result: Showed no PI nuclear localization at 1 h; exhibited prominent red fluorescence (PI entry) in nuclei at 6 h, indicating late-stage apoptosis, with nearly complete PI nuclear localization after longer incubation.

Apoptosis Analysis[1]

Cell Line: human lung cancer A549 cells, normal human liver L02 cells
Concentration: 1 μM, 2 μM
Incubation Time: 48 h
Result: Induced significant apoptosis in A549 cells, with 14.5% early apoptosis and 49.0% late apoptosis at 2 μM.
Induced no significant apoptosis in L02 cells.

Cell Cycle Analysis[1]

Cell Line: human lung cancer A549 cells, normal human liver L02 cells
Concentration: 1 μM, 2 μM
Incubation Time: 24 h
Result: Arrested the cell cycle of A549 cells at the G0/G1 phase, with no significant effect on L02 cell cycle distribution.
分子量

633.15

Formula

C40H38ClO3P

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
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  • 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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产品名称:
Mito-DHH chloride
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HY-181525
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