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编 号:F597829
分子式:C15H10O4
分子量:254.24
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10mM*1mL in DMSO
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5mg
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10mg
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生物活性:
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.

体内研究:
SKI V (75 mg/kg; i.p.; 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:IP; days 1, 5, 9, 15
Result:Tumor growth was significantly lower (>50% decreased at day 18) than tumor growth in control animals.

体外研究:
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.
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