Mensacarcin

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Mensacarcin 

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。

Mensacarcin

Mensacarcin Chemical Structure

CAS No. : 808750-39-2

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生物活性

Mensacarcin, a highly complex polyketide, strongly inhibits cell growth universally in cancer cell lines and potently induces apoptosis in melanoma cells. Mensacarcin targets to mitochondria, affects energy metabolism in mitochondria, and activates caspase-dependent apoptotic pathways. Mensacarcin, an antibiotic, can be used as a cytotoxic component of antibody-drug conjugates (ADCs)[1][2].

IC50 & Target

Traditional Cytotoxic Agents

 

体外研究
(In Vitro)

Mensacarcin (0-100 μM; 24 hours) exhibits general cytostatic but type-specific cytotoxic effects for melanoma cells[1].
Mensacarcin (2-50 μM; 15 hours) induces rapid apoptotic cell death in melanoma cells[1].
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[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

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[1]

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.

分子量

420.41

Formula

C21H24O9
CAS 号

808750-39-2
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.
参考文献

  • [1]. Birte Plitzko, et al. The natural product mensacarcin induces mitochondrial toxicity and apoptosis in melanoma cells. J Biol Chem. 2017 Dec 22;292(51):21102-21116.

    [2]. Lutz F. Tietze, et al. Intramolecular Heck Reactions for the Synthesis of the Novel Antibiotic Mensacarcin: Investigation of Catalytic, Electronic and Conjugative Effects in the Preparation of the Hexahydroanthracene Core. Chemistry Europe. Volume2005, Issue9.

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