SKI-178 is a selective inhibitor of sphingosine kinase 1 which is active in vitro and in vivo. SKI-178 is a competitive inhibitor of sphingosine binding to SPHK1 (Ki = 1.3 uM) and shows no inhibition of SPHK2 up to 25 uM. SKI-178 is cytotoxic to numerous cancer cell lines (MCF-7, A549, Panc-1, etc) at low to sub-micromolar concentrations.
| Categories | Biochemical Reagents |
|---|---|
| Filter | Inhibitor, Sphingolipid |
| CAS Number | 1259484-97-3 |
| Molecular Formula | C21H22N4O4 |
| Molecular Weight (g/mol) | 394.43 |
| Purity | 0.95 |
| Storage | -20 °C or below |
| Shipping Temp | Room Temperature |
1) J.A. Hengst et al. “Development of a sphingosine kinase 1 specific small-molecule inhibitor” Bioorg. Med. Chem. Lett. 2010, 20, 7498-7502. doi: 10.1016/j.bmcl.2010.10.005
2) T.E. Dick et al. “The apoptotic mechanism of action of the sphingosine kinase 1 selective inhibitor SKI-178 in human acute myeloid leukemia cell lines” J. Pharmacol. Exp. Ther. 2015, 352, 494-508. doi: 10.1124/jpet.114.219659
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