SKI V

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SKI V 是一种有效的非竞争性非脂质鞘氨醇激酶 (SPHK; SK) 抑制剂 (GST-hSK,IC50 : 2 μM)，也是一种 PI3K 抑制剂 (hPI3k,IC50 : 6 μM)，诱导细胞凋亡并具有抗肿瘤活性

SKI V is a potent and noncompetitive non-lipid sphingosine kinase (SPHK; SK) inhibitor (GST-hSK,IC50 : 2 μM), and is a PI3K inhibitor(hPI3k,IC50 : 6 μM), induces apoptosis and has antitumor activity.

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. Cell Proliferation Assay Cell Line:T24 tumor cells Concentration:10 μM Incubation Time:For 24 hours Result:Inhibited cancer cell proliferation.Apoptosis Analysis Cell Line:T24 tumor cells Concentration:10 μM Incubation Time:For 24 hours Result:Induced apoptosis.Western Blot AnalysisCell Line:JC cells Concentration:0.2, 1, 5 μM Incubation Time:Pretreated for 1 hour Result:Decreased phospho-Akt and phospho-MEK levels.

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 cellsDosage: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.

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GPCR/G Protein

S1P Receptor

SphK|PI3K

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24418-86-8

254.24

C15H10O4

>98% (HPLC)

In Vitro:?DMSO : 50 mg/mL (196.66 mM)

Oc1ccc(\C=C2\Oc3ccccc3C2=O)cc1O

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(-20℃)

With Ice Pack

≥ 2 years