567731
Sphingosine Kinase Inhibitor
The Sphingosine Kinase Inhibitor, also referenced under CAS 1177741-83-1, controls the biological activity of Sphingosine Kinase. This small molecule/inhibitor is primarily used for Cell Signaling applications.
别名:
Sphingosine Kinase Inhibitor, 2-( p-Hydroxyanilino)-4-( p-chlorophenyl) thiazole, HCl, SK Inhibitor I, 2-(p-Hydroxyanilino)-4-(p-chlorophenyl) thiazole, HCl, SK Inhibitor I
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关于此项目
经验公式（希尔记法）:
C15H11ClN2OS · xHCl
化学文摘社编号:
分子量:
302.78 (free base basis)
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77
质量水平
方案
≥98% (HPLC)
表单
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
desiccated (hygroscopic)
protect from light
颜色
white
溶解性
DMSO: 5 mg/mL
运输
ambient
储存温度
2-8°C
SMILES字符串
[s]1c(nc(c1)c3ccc(cc3)Cl)Nc2ccc(cc2)O.Cl
InChI
1S/C15H11ClN2OS.ClH/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);1H
InChI key
ZDRVLAOYDGQLFI-UHFFFAOYSA-N
相关类别
一般描述
A cell-permeable disubstituted thiazole compound that displays anti-tumor properties. Acts as a potent, substrate competitive, reversible, and highly specific inhibitor of sphingosine kinase (IC50 = 0.5 µM for GST-hSK). Does not affect the kinase activity of hERK2, hPI3K, or PKCα even at concentrations as high as 60 µM. Induces apoptosis in human cancer cells that express the drug transport proteins Pgp or MRP1 (IC50 = ~ 1-5 µM) through inhibiting sphingosine-1-phosphate production.
A cell-permeable, potent non-ATP-competitive, reversible, and specific inhibitor of sphingosine kinase (IC50 = 500 nM for GST-hSK) that also exhibits anti-tumor properties. Does not affect the kinase activity of hERK2, hPI3 K, or PKCα at cocentrations as high as 60 µM. Shown to induce apoptosis in human cancer cells that express the drug transport proteins Pgp or MRP1 (IC50 ~1-5 µM) by inhibiting sphingosine-1-phosphate production.
生化/生理作用
Cell permeable: yes
Primary Target
GST-hsk
GST-hsk
Product competes with ATP.
Reversible: yes
Target IC50: 0.5 µM for GST-hSK
包装
Packaged under inert gas
制备说明
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
French, K.J., et al. 2003. Cancer Res.63, 5962.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
免责声明
Toxicity: Carcinogenic / Teratogenic (D)
储存分类代码
11 - Combustible Solids
WGK
WGK 1
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iScience, 24(11), 103351-103351 (2021-11-23)
The importance of the G-protein βγ subunits in the regulation of cargo transport from the trans-Golgi network (TGN) to the plasma membrane (PM) is well accepted; however, the molecular mechanism underlying the G-protein activation at the TGN remains unclear. We
Mahesh Yadav et al.
Journal of immunology (Baltimore, Md. : 1950), 176(9), 5494-5503 (2006-04-20)
Previous studies have shown that the ability of Mycobacterium tuberculosis to block a Ca(2+) flux is an important step in its capacity to halt phagosome maturation. This affect on Ca(2+) release results from M. tuberculosis inhibition of sphingosine kinase (SPK)
Ilari Pulli et al.
Biochimica et biophysica acta, 1853(9), 2173-2182 (2015-04-22)
Caveolae are plasma membrane invaginations enriched in sterols and sphingolipids. Sphingosine kinase 1 (SK1) is an oncogenic protein that converts sphingosine to sphingosine 1-phosphate (S1P), which is a messenger molecule involved in calcium signaling. Caveolae contain calcium responsive proteins, but
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