SKI II

半岛bd体育手机客户端 说明

应用

SKI II has been used to study the regulatory mechanism and signaling pathway induced by SKI II in inhibiting tumor growth.
Human cisplatin-resistant gastric cancer cell line was treated with SKI-II to study the mechanism of reversion of multidrug resistance.¹

包装

10, 50 mg in glass bottle

生化/生理作用

Sphingosine kinase (SK) plays a pivotal role in regulating tumor growth and SK can act as an oncogene. Expression of SK RNA is significantly elevated in a variety of solid tumors, compared with normal tissue from the same patient. A number of novel inhibitors of human SK were identified, and several representative compounds were characterized in detail. These compounds demonstrated activity at sub- to micromolar concentrations, making them more potent than any other reported SK inhibitor, and were selective toward SK compared with a panel of human lipid and protein kinases. Kinetic studies revealed that the compounds were not competitive inhibitors of the ATP-binding site of SK. 4-[4-(4-chloro-phenyl)-thiazol-2-ylamino]-phenol (SKI-II) inhibitor is orally bioavailable, detected in the blood for at least 8 h, and showed a significant inhibition of tumor growth in mice with IC₅₀= 0.5 μM; SKI II does not act at ATP-binding site. Displays no inhibition of ERK2, PI 3-kinase, or PKCa at concentrations up to 60 μM.SKI II induces apoptosis and inhibits proliferation in several other tumor cell linesin vitro(IC₅₀= 0.9-4.6 μM).

特点和优势

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

其他说明

Product is air and light sensitive

基本信息

经验(实验)分子式	C15H11ClN2OS
分子量	302.78
MDL编号	MFCD00733553
PubChem化学物质编号	24724614
NACRES	NA.77

半岛bd体育手机客户端 性质

质量水平	100
测定	≥98% (HPLC)
形式	solid
储存条件	protect from light
颜色	off-white
溶解性	DMSO: ≥20 mg/mL
储存温度	2-8℃
SMILES string	Oc1ccc(Nc2nc(cs2)-c3ccc(Cl)cc3)cc1
InChI	1S/C15H11ClN2OS/c16-11-3-1-10(2-4-11)14-9-20-15(18-14)17-12-5-7-13(19)8-6-12/h1-9,19H,(H,17,18)
InChI key	ZFGXZJKLOFCECI-UHFFFAOYSA-N

安全信息

储存分类代码	13 - Non Combustible Solids
WGK	WGK 3
闪点(F)	Not applicable
闪点(C)	Not applicable
个人防护装备	Eyeshields, Gloves, type N95 (US)