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.
References
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 |
|---|
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