SKI II

An SPHK1 inhibitor

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库存: 现货

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数量
25mg

￥862.00

690.00

- +
100mg

￥3125.00

2500.00

- +
500mg

￥13462.00

10770.00

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1g

￥23187.00

18550.00

- +

已选 0 种 0 瓶

金额: ￥0.00

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Background

SKI II is an inhibitor of sphingosine kinase with IC50 value of 0.5μM[1].

SKI II is selective against SK and has no inhibition of human protein kinases ERK2, PKC-I and the lipid kinase PI3K. It is reported that SKI II is not a competitive inhibitor at the ATP-binding site of SK. SKI II also inhibits endogenous SK in intact MDA-MB-231 cells [1].

As a SK inhibitor, SKI II prevents SK from catalyzing the generation of sphingosine 1-phosphate (S1P). The blockage of S1P formation leads to inhibition of proliferation, as well as the induction of apoptosis in cancer cells. SKI II shows cytotoxicity in T-24 human bladder carcinoma cells, MCF-7 human breast adenocarcinoma cells and the subline of MCF-7 cells, MCF-7/VP, with IC50 values of 4.6μM, 1.2μM and 0.9μM, respectively [1].

参考文献:
[1] French KJ, Schrecengost RS, Lee BD, Zhuang Y, Smith SN, Eberly JL, Yun JK, Smith CD. Discovery and evaluation of inhibitors of human sphingosine kinase. Cancer Res. 2003 Sep 15;63(18):5962-9.