SKI II

CAS号

312636-16-1

分子式

C15H11ClN2OS

主要靶点

Apoptosis|S1P Receptor|Wnt/beta-catenin

仅限科研使用

Cat No : CM06514

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Synonyms

S1P Receptor|S1PReceptor|SKI II|Sphingosine kinase|SphK-I2|SphK|SphK1|βcatenin|Wnt|Wnt/b-catenin|Wnt/betacatenin|Wnt/β-catenin|inhibit|Inhibitor|bcatenin|beta-catenin|betacatenin|Apoptosis



产品信息

CAS号 312636-16-1
分子式 C15H11ClN2OS
主要靶点 Apoptosis|S1P Receptor|Wnt/beta-catenin
主要通路 干细胞|细胞骨架|G 蛋白偶联受体|凋亡
分子量 302.78
纯度 99.93%, 此纯度可做参考,具体纯度与批次有关系,可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
别名 S1P Receptor|S1PReceptor|SKI II|Sphingosine kinase|SphK-I2|SphK|SphK1|βcatenin|Wnt|Wnt/b-catenin|Wnt/betacatenin|Wnt/β-catenin|inhibit|Inhibitor|bcatenin|beta-catenin|betacatenin|Apoptosis

靶点活性

SPHK:0.5 μM

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。

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.

溶解度

DMSO:40 mg/mL (132.11 mM)

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)

参考文献

1.French KJ, et al. Cancer Res, 2003, 63(18), 5962-5969.
2.French KJ, et al. J Pharmacol Exp Ther, 2006, 318(2), 596-603.
3.Zhu ZA, et al. Asian Pac J Cancer Prev, 2012, 13(2), 625-631.
4.Chiba Y, et al. J Pharmacol Sci, 2010, 114(3), 304-310.
5.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.

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