SKI-II is a commonly used inhibitor of both sphingosine kinase I (SPHK1) and 2 (SPHK2). Recently it has been shown to inhibit dihydroceramide desaturase (Des1) which Aurelio et al. suggest is actually responsible for its anti-proliferative activity, not SPHK inhibition. Compound 34 is an analog of SKI-II and is a selective Des1 inhibitor which shows no activity against either SPHK1 or SPHK2. 34 inhibits PC3 cell growth (GIC50 = 0.34 μM) but some of this may be due to inhibition of another target
References
Powered by Bioz See more details on BiozL. Aurelio, C.V. Scullino, et al.. “From Sphingosine Kinase to Dihydroceramide desaturase: A Structure?Activity Relationship (SAR) Study of the Enzyme Inhibitory and Anticancer Activity of 4-((4-(4-Chlorophenyl)thiazol-2-yl)amino)phenol (SKI-II)” J. Med. Chem., 59, 965-984, DOI: 10.1021/acs.jmedchem.5b01439.
| Categories | Biochemical Reagents |
|---|---|
| Filter | Inhibitor, Sphingolipid |
| CAS Number | 1847471-67-3 |
| Molecular Formula | C15H12ClN5O2 |
| Molecular Weight (g/mol) | 329.74 |
| Purity | 95% |
| Storage | 4 °C or below |
