MENSACARCIN
- CAS号:808750-39-2
- 英文名:Mensacarcin
- 中文名:MENSACARCIN
- CBNumber:CB82650838
- 分子式:C21H24O9
- 分子量:420.40986
- MOL File:808750-39-2.mol
- 沸点 :656.8±55.0 °C(Predicted)
- 密度 :1.53±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO: soluble,Methanol: soluble
- 形态 :A solid
- 酸度系数(pKa) :11.50±0.70(Predicted)
- 颜色 :White to off-white
MENSACARCIN性质、用途与生产工艺
- 生物活性 Mensacarcin 是一种高度复杂的聚酮类化合物，在肿瘤细胞系中普遍具有强烈的抑制细胞生长的作用，并可能诱导黑色素瘤细胞的凋亡 (apoptosis)。Mensacarcin 靶向线粒体 (mitochondria)，影响线粒体的能量代谢，激活 caspase 依赖的凋亡途径。Mensacarcin 是一种抗生素，也可作为抗体偶联药物 (ADCs) 的细胞毒性成分。
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靶点
Traditional Cytotoxic Agents
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体外研究
Mensacarcin (0-100 μM; 24 hours) exhibits general cytostatic but type-specific cytotoxic effects for melanoma cells.
Mensacarcin (2-50 μM; 15 hours) induces rapid apoptotic cell death in melanoma cells.
Mensacarcin exhibits potent cytostatic properties (mean of 50% growth inhibition=0.2 μM) in almost all cell lines of the National Cancer Institute (NCI)-60 cell line screen and relatively selective cytotoxicity against melanoma cells. Mensacarcin is a highly oxygenated polyketide that was first isolated from soil-dwelling Streptomyces bacteria. Mensacarcin impairs mitochondrial function in melanoma cells.Cell Viability Assay
Cell Line: SK-Mel-28 and SK-Mel-5 melanoma cells, HCT-116 colon cancer cells Concentration: 0.01, 0.1, 1, 10, 100 μM Incubation Time: 24 hours Result: Induced concentration- and time-dependent cell death in the two tested melanoma cell lines. HCT-116 colon carcinoma cells were strongly inhibited. Western Blot Analysis
Cell Line: SK-Mel-28, SK-Mel-5 cells Concentration: 2, 10, 50 μM Incubation Time: 15 hours Result: Induced the formation of 89-kDa PARP-1 fragments as well as caspase-3 activation in SK-Mel-28 and SK-Mel-5 beginning between 6 and 15 h after exposure.
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