SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC50 of 2 μM for GST-hSK. SKI V potently inhibits PI3K with an IC50 of 6 μM for hPI3k. SKI V decreases formation of the mitogenic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity[1][2].
ChEBI: 3',4'-dihydroxyaurone is a hydroxyaurone that is aurone which is substituted by hydroxy groups at the 3' and 4' positions; major species at pH 7.3. It shows inhibitory activity against several isoforms of the histone deacetylase complex (HDAC). It has a role as an EC 3.5.1.98 (histone deacetylase) inhibitor. It is a hydroxyaurone and a member of catechols. It is functionally related to a 2',3,4-trihydroxy-trans-chalcone.
SKI V is a non-competitive, potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with IC50 of 2 μM against GST-hSK. SKI V potently inhibits PI3K with IC50 of 6 μM for hPI3k. SKI V reduces the formation of the mitotic second messenger sphingosine-1-phosphate (S1P). SKI V induces apoptosis and has antitumor activity.
SKI V (75 mg/kg; ip; days 1, 5, 9, 15) significantly lowers tumor growth (>50% decreased at day 18) than control animals.
| Animal Model: | 6-8 weeks old BALB/c female mice with JC mammary adenocarcinoma cells |
| Dosage: | 75 mg/kg |
| Administration: | < td class="col2"> IP; days 1, 5, 9, 15
| Result: | Tumor growth was significantly lower (>50% decreased at day 18) than tumor growth in control animals. |
IC50: 2 μM (GST-hSK), 6 μM (hPI3k) and 80 μM (ERK2)
[1] French KJ, et al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9. PMID:14522923
[2] French KJ, et al. Antitumor activity of sphingosine kinase inhibitors. J Pharmacol Exp Ther. 2006 Aug;318(2):596-603. DOI:
10.1124/jpet.106.101345
