SKI II

产品编号 T6673   CAS 312636-16-1
别名: SphK-I2, SphK-I2

SKI II is a highly selective and non-ATP-competitive S1P receptor inhibitor (IC50: 0.5 μM) while exhibiting no inhibitory action on other kinases including PKCα, PI3K, and ERK2.

SKI II结构式
SKI II , CAS 312636-16-1
规格 库存 价格/RMB 数量
5 mg 上海现货 489.00
10 mg 上海现货 632.00
25 mg 上海现货 1107.00
50 mg 上海现货 1962.00
100 mg 上海现货 3482.00
200 mg 待询 6237.00
1 mL * 10 mM (in DMSO) 上海现货 489.00
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生物活性
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存储 & 溶解度
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产品描述 SKI II is a highly selective and non-ATP-competitive S1P receptor inhibitor (IC50: 0.5 μM) while exhibiting no inhibitory action on other kinases including PKCα, PI3K, and ERK2.
靶点活性 SphK1 : ic50 0.5μM,  
Kinase Assay SK Assay: A medium-throughput assay suitable for screening for inhibitors of recombinant human SK has been established. Briefly, 5 μg of purified GST-SK fusion protein are combined with 12 nM sphingosine, which contains a 100-fold dilution of [3-3H]sphingosine (20 Ci/mmol), 1 mM ATP, 1 mM magnesium chloride, and 200 μL of assay buffer [20 mM Tris HCl (pH 7.4), 20% glycerol, 1 mM beta-mercaptoethanol, 1 mM EDTA, 20 mM zinc chloride, 1 mM sodium orthovanadate, 15 mM sodium fluoride, and 0.5 mM 4-deoxypyridoxine]. Assays are run for 30 min at 25°C with shaking and contains either 1% DMSO or 5 g/mL test compound, which corresponds to concentrations of 10–25 μM. The reactions are terminated with 50 μL of concentrated ammonium hydroxide, followed by extraction of the assay mixture with chloroform:methanol (2:1). The aqueous portion is transferred to scintillation vials and radioactivity is quantified as a measure of [3H]]S1P formation using a Beckman LS 3801 Scintillation Counter. The intra-assay coefficient of variation is ~10%, whereas interassay variation is ~20%.
Cell Research
T24, MCF-7, MCF-7/VP, and NCI/ADR cells are plated into 96-well tissue culture plates at ~15% confluency. After 24 hours, cells are treated with various concentrations of inhibitors. After an additional 48 hours, cell survival is assayed using the sulforhodamine B assay.(Only for Reference)
Cell lines: T-24, MCF-7, MCF-7/VP, NCI/ADR cell lines
Animal Research
Animal Model: JC xenografts are established in mice
别名 SphK-I2, SphK-I2
纯度 99.93%
分子量 302.78
分子式 C15H11ClN2OS
CAS No. 312636-16-1

存储

0-4℃ for short term (days to weeks), or -20℃ for long term (months).

溶解度

DMSO: 30.3 mg/mL (100 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

Solution 1

30% PEG400+0.5% Tween80+5% propylene glycol: 20 mg/mL

文献引用

参考文献
6. Liu H, et al. SphK1 inhibitor SKI II inhibits the proliferation of human hepatoma HepG2 cells via the Wnt5A/β-catenin signaling pathway. Life Sci. 2016 Apr 15;151:23-9.

Related Compound Libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Inhibitor Library Anti-cancer Compound Library Protease Inhibitor Library Immunology/Inflammation Compound Library Kinase Inhibitor Library GPCR Compound Library

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