神經酰胺是一種具有生物活性的鞘脂，可誘導細胞凋亡。神經酰胺酶（CD酶）水解脂肪酸鏈，保持神經酰胺水平在檢查中，并已提出作為抗癌治療的小分子抑制劑的目標。Ceranib-2在SKOV 3細胞中以IC 50 = 28 uM抑制細胞CD酶活性，并且在高達100 uM時未顯示出顯著的細胞毒性。SKOV 3細胞與Ceranib-2孵育導致所有神經酰胺物質增加，鞘氨醇和S1 P呈劑量依賴性降低。Ceranib-2抑制皮下JC細胞腫瘤小鼠模型中的腫瘤生長。參考文獻1）J.M德雷珀等人“人類神經酰胺酶抑制劑的發現和評價”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.生物化學研究通訊2015年464 833-839。
產品描述
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.
