Ceranib-2（神經(jīng)酰胺酶抑制劑）-Ceranib-2 (Ceramidase inhibitor)代理/參數(shù)/廠家-其它-艾美捷科技有限公司

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背景資料: 神經(jīng)酰胺是一種具有生物活性的鞘脂，可誘導(dǎo)細(xì)胞凋亡。神經(jīng)酰胺酶（CD酶）水解脂肪酸鏈，保持神經(jīng)酰胺水平在檢查中，并已提出作為抗癌治療的小分子抑制劑的目標(biāo)。Ceranib-2在SKOV 3細(xì)胞中以IC 50 = 28 uM抑制細(xì)胞CD酶活性，并且在高達(dá)100 uM時(shí)未顯示出顯著的細(xì)胞毒性。SKOV 3細(xì)胞與Ceranib-2孵育導(dǎo)致所有神經(jīng)酰胺物質(zhì)增加，鞘氨醇和S1 P呈劑量依賴性降低。Ceranib-2抑制皮下JC細(xì)胞腫瘤小鼠模型中的腫瘤生長(zhǎng)。參考文獻(xiàn)1）J.M德雷珀等人“人類神經(jīng)酰胺酶抑制劑的發(fā)現(xiàn)和評(píng)價(jià)”Mol.癌癥治療2011年10月2052-20612）Vethakanraj等人，“Targeting ceramide metabolic pathway induces apoptosis in human breast cancer cell lines”Biophys.生物化學(xué)研究通訊2015年464 833-839。

產(chǎn)品描述: Ceramides are bioactive sphingolipids which induce apoptosis in cells. Ceramidases (CDase) which hydrolyze the fatty acid chain keep ceramide levels in check and have been proposed as a target for small-molecule inhibitors for anti-cancer therapy. Ceranib-2 inhibits cellular CDase activity with an IC50 = 28 uM in SKOV3 cells and does not show significant cytotoxity up to 100uM. Incubations of SKOV3 cells with Ceranib-2 resulted in an increase in all ceramide species and a dose-dependant decrease in sphingosine and S1P. Ceranib-2 suppressed tumor growth in a mouse model with subcutaneous JC cell tumors.References1) J.M Draper et al. "Discovery and Evaluation of Inhibitors of Human Ceramidase" Mol. Cancer Ther. 2011 10 2052-20612) H.S. Vethakanraj et al. "Targeting ceramide metabolic pathway induces apoptosis in human breast cancer cell lines" Biophys. Biochem. Res. Commun. 2015 464 833-839.

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