S5696
SKI II
≥98% (HPLC), selective non-lipid sphingosine kinase (SK) inhibitor, solid
别名:
4-[[4-(4-Chlorophenyl)-2-thiazolyl]amino]phenol
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关于此项目
经验公式（希尔记法）:
C15H11ClN2OS
化学文摘社编号:
分子量:
302.78
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77
MDL number:
产品名称
SKI II, ≥98% (HPLC), solid
SMILES string
Oc1ccc(Nc2nc(cs2)-c3ccc(Cl)cc3)cc1
InChI key
ZFGXZJKLOFCECI-UHFFFAOYSA-N
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)
assay
≥98% (HPLC)
form
solid
storage condition
protect from light
color
off-white
solubility
DMSO: ≥20 mg/mL
storage temp.
2-8°C
Quality Level
Application
Human cisplatin-resistant gastric cancer cell line was treated with SKI-II to study the mechanism of reversion of multidrug resistance.1
SKI II has been used to study the regulatory mechanism and signaling pathway induced by SKI II in inhibiting tumor growth.
Biochem/physiol Actions
SKI II is a selective non-lipid sphingosine kinase (SK) inhibitor. IC50 = 0.5 μM; does not act at ATP-binding site. Displays no inhibition of ERK2, PI 3-kinase, or PKCα at concentrations up to 60 μM. Induces apoptosis and inhibits proliferation in several other tumor cell lines in vitro (IC50 = 0.9-4.6 μM).
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 lines in vitro (IC50 = 0.9-4.6 μM).
Features and Benefits
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.
Other Notes
Product is air and light sensitive
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
ppe
Eyeshields, Gloves, type N95 (US)
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SphK1 inhibitor SKI II inhibits the proliferation of human hepatoma HepG2 cells via the Wnt5A/beta-catenin signaling pathway
Liu H, et al.
Life Sciences, 151, 23-29 (2016)
Bo Kyung A Seong et al.
Cancer research, 77(3), 696-706 (2016-12-03)
Metastatic relapse is the major cause of death in pediatric neuroblastoma, where there remains a lack of therapies to target this stage of disease. To understand the molecular mechanisms mediating neuroblastoma metastasis, we developed a mouse model using intracardiac injection
Zu-An Zhu et al.
Asian Pacific journal of cancer prevention : APJCP, 13(2), 625-631 (2012-04-25)
In order to investigate whether SKI-II could reverse drug resistance and its possible mechanisms, we treated SGC7901/DDP cells with SKI-II or SKI-II in combination with DDP. Then cell growth, apoptosis, micro- morphological changes, and expression of SphK1, P-gp, NF-kB, Bcl-2
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