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SKI II
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产品介绍
产品介绍
产品信息
抗原名称
Sphingosine Kinase
商品描述
SKI II是一种高度选择性的，非ATP竞争性的S1P receptor抑制剂，IC50为0.5 μM，对其他激酶，包括PI3K， PKCα和ERK2没有抑制作用。SKI II作用于乳腺癌细胞系MDA-MB-231，有效抑制内源性SK活性。SKI II作用于人类癌细胞系，包括T-24, MCF-7, MCF-7/VP, NCI/ADR，具有显著的抗增殖效果，IC50分别为4.6 μM, 1.2 μM, 0.9 μM 和 1.3 μM。SKI II也诱导T24细胞凋亡，与降低S1P水平相一致。
分子量
302.78
纯度
>98%
可溶性
DMSO ：30.3 mg/mL (100 mM)
外观
类白色粉末
In vitro(体外研究)
SKI II potently inhibits endogenous SK activities in the breast cancer cell line MDA-MB-231. SKI II demonstrates significantly antiproliferative effects in human cancer cell lines including T-24, MCF-7, MCF-7/VP, NCI/ADR with IC50 of 4.6 μM , 1.2 μM, 0.9 μM and 1.3 μM, respectively. SKI II also induces apoptosis of T24 cells consistent with the hypothesized consequence of reducing S1P levels. As demonstrated previously in MDA-MB-231 cells, SKI II decreases S1P formation in JC cells in a concentration-dependent manner, with IC50 of 12 μM. In addition, SKI-II can reverse drug resistance of SGC7901/DDP to cisplatin by down-regulating expression of P-gp and up-regulating apoptosis through down-regulation of SphK1.
In vivo(体内研究)
SKI II (50 mg/kg) after intraperitoneal or oral administration significantly decreases tumor growth a syngeneic Balb/c mouse solid tumor model that uses JC mammary adenocarcinoma cells relative to control groups with no overt toxicity or weight loss. SKI-II (50 mg/kg ip) ameliorates antigen-induced bronchial smooth muscle hyperresponsiveness in mice by endogenously inhibiting generation of S1P.
背景
别名
SphK-I2；鞘氨醇激酶抑制剂
分子式
C15H11ClN2OS
CAS号
312636-16-1
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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