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SKI II
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
SKI II图片
CAS NO:312636-16-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
25mg电议
100mg电议
500mg电议
1g电议

产品介绍
SKI-II 是一种口服活性和合成的鞘氨醇激酶 (SK) 活性抑制剂,对 SK1 和 SK2 的 IC50 值分别为 78 μM 和 45 μM。 SKI II 通过诱导其溶酶体和/或蛋白酶体降解对 SK1 造成不可逆的抑制。
Cas No.312636-16-1
别名鞘氨醇激酶抑制剂
化学名4-[[4-(4-chlorophenyl)-1,3-thiazol-2-yl]amino]phenol
Canonical SMILESC1=CC(=CC=C1C2=CSC(=N2)NC3=CC=C(C=C3)O)Cl
分子式C15H11ClN2OS
分子量302.78
溶解度≥ 15.15mg/mL in DMSO
储存条件Store at -20° C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

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].

References:
[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.