Powder: -20°C for 3 years | In solvent: -80°C for 1 year
SKI II (SphK-I2) 是一种口服有效的合成鞘氨醇激酶 (SK)抑制剂,抑制 SK1 和 SK2,IC50值分别为 78 μM 和 45 μM。它通过诱导溶酶体/蛋白酶体降解,不可逆地抑制SK1。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 186 | 现货 | ||
5 mg | ¥ 418 | 现货 | ||
10 mg | ¥ 575 | 现货 | ||
25 mg | ¥ 987 | 现货 | ||
50 mg | ¥ 1,690 | 现货 | ||
100 mg | ¥ 2,970 | 现货 | ||
200 mg | ¥ 4,550 | 现货 | ||
500 mg | ¥ 6,950 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 443 | 现货 |
产品描述 | SKI II (SphK-I2) 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 | SPHK:0.5 μM |
体外活性 | SKI II(50 mg/kg,i.p.)通过抑制小鼠内源性1-磷酸鞘氨醇生成,可改善抗原诱导的支气管平滑肌高反应性.在携带JC乳腺癌细胞的同源Balb/c小鼠实体瘤模型中, SKI II(50 mg/kg,i.p./p.o.)可显著降低肿瘤生长,与对照组相比,无明显的毒性或体重减轻. |
体内活性 | 与降低S1P水平一致,SKI II可诱导T24细胞凋亡。在JC细胞中,SKI II可浓度依赖性降低S1P形成(IC50:12 μM)。在乳腺癌细胞系MDA-MB-231中,SKI II可明显抑制内源性SK活性。在人类癌细胞系,包括T-24,MCF-7,MCF-7/VP,NCI/ADR中,SKI II均有显著的抗增殖效果(IC50:4.6/1.2/0.9/1.3 μM)。此外,通过下调P-gp的表达,及通过下调SPHK1而上调凋亡,SKI II可逆转SGC7901/DDP对顺铂的耐药性。 |
激酶实验 | 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%. |
细胞实验 | 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) |
别名 | SphK-I2 |
分子量 | 302.78 |
分子式 | C15H11ClN2OS |
CAS No. | 312636-16-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 30.3 mg/mL (100 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 3.3027 mL | 16.5136 mL | 33.0273 mL | 82.5682 mL |
5 mM | 0.6605 mL | 3.3027 mL | 6.6055 mL | 16.5136 mL | |
10 mM | 0.3303 mL | 1.6514 mL | 3.3027 mL | 8.2568 mL | |
20 mM | 0.1651 mL | 0.8257 mL | 1.6514 mL | 4.1284 mL | |
50 mM | 0.0661 mL | 0.3303 mL | 0.6605 mL | 1.6514 mL | |
100 mM | 0.033 mL | 0.1651 mL | 0.3303 mL | 0.8257 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
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