SKI V 是一种非竞争性的，有效的非脂质鞘氨醇激酶 (SPHK; SK) 抑制剂，对 GST-hSK 的 IC₅₀ 为 2 μM。 SKI V 有效抑制 PI3K，对 hPI3k 的 IC₅₀ 为 6 μM。SKI V 减少有丝分裂的第二信使鞘氨醇-1-磷酸 (S1P) 的形成。SKI V 诱导细胞凋亡 (apoptosis) 并具有抗肿瘤活性。

SKI V is a noncompetitive and potent non-lipid sphingosine kinase (SPHK; SK) inhibitor with an IC 50 of 2 μM for GST-hSK. SKI V potently inhibits PI3K with an IC 50 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.

Solid

IC50: 2 μM (GST-hSK), 6 μM (hPI3k) and 80 μM (ERK2)

SKI V has weak activity toward ERK2 (IC50 of 80 μM for hERK2) and does not inhibit PKC-α.
SKI V (10 μM; for 24 hours) inhibits cancer cell proliferation and induces apoptosis.
SKI V (0.2, 1, 5 μM; pretreated for 1 hour) decreases phospho-Akt and phospho-MEK levels. Near-confluent cultures of JC cells are serum-starved for 16 hours, followed by pretreatment SKI V for 1 hour.
SKI V has IC50s for inhibition of sphingosine kinase (SK) and tumor cell proliferation of ～2 μM.
SKI V (20 μg/ml) inhibits not only purified but endogenous SK in in MDA-MB-231 cells.
SKI V (0.2, 1, 5 μM) inhibits intracellular S1P formation in JC cells in a dose-dependent fashion.
has not independently confirmed the accuracy of these methods. They are for reference only.

SKI V (75 mg/kg; i.p.; days 1, 5, 9, 15) significantly lowers tumor growth (>50% decreased at day 18) than control animals. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: 6-8 week

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. French KJ, et al. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9.
[2]. French KJ, et al. Antitumor activity of sphingosine kinase inhibitors. J Pharmacol Exp Ther. 2006 Aug;318(2):596-603.

In Vitro: DMSO : 50 mg/mL (196.66 mM; Need ultrasonic)配制储备液