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.
1) 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.
Categories | Biochemical Reagents |
---|---|
Filter | Inhibitor, Sphingolipid |
CAS Number | 1402830-75-4 |
Molecular Formula | C25H19NO3 |
Molecular Weight (g/mol) | 381.42 |
Purity | >98% |
Storage | -20 °C or below |
Echelon-脂类研究的最佳拍档
Echelon是脂质研究和脂质与蛋白质相互作用研究领域的引导者。脂质蛋白相互作用是众多的细胞信号通路钟高级调控必不可少的。异常的细胞信号通路将会导致许多疾病,例如癌症、炎症、糖尿病和心血管疾病等。Echelon一直是脂质研究信息,脂质信号分析的顶级供应商。