货号 | 13371-1mg |
描述 | The sphingosine kinases (SPHK) phosphorylate sphingosine, producing the important lipid mediator sphingosine-1-phosphate (S1P). The two known kinases, SPHK 1 and SPHK 2, have different developmental and tissue expression patterns, suggesting that they have distinct physiological functions.1,2 Notably, SPHK 1 is overexpressed in several forms of cancer and inhibition of SPHK 1 inhibits tumor growth.3 CAY10621 is a selective inhibitor of SPHK 1, both in vitro(IC50 = 3.3 μM) and in U937 cells overexpressing human SPHK 1 (70% inhibition at 5 μM).4 It has no inhibitory effect on SPHK 2 either in vitro or in cells. Similarly, CAY10621 does not reduce the activity of protein kinase C (PKC) except at very high concentration (>75 μM).4 |
别名 | SKI 5C;SPHK 1 Inhibitor 5C; |
供应商 | Cayman |
应用文献 | |
1.Spiegel, S., and Milstien, S. Functions of the multifaceted family of sphingosine kinases and some close relatives. The Journal of Biological Chemisty 282(4), 2125-2129 (2007). 2.Takabe, K.,Paugh, S.W.,Milstien, S., et al. "Inside-out" signaling of sphingosine-1-phosphate: Therapeutic targets. Pharmacological Reviews 60, 181-195 (2008). 3.Shida, D.,Takabe, K.,Kapitonov, D., et al. Targeting SphK1 as a new strategy against cancer. Current Drug Targets 9(8), 662-673 (2008). 4.Wong, L.,Tan, S.L.,Lam, Y., et al. Synthesis and evaluation of sphingosine analogues as inhibitors of sphingosine kinases. Journal of Medicinal Chemistry 52, 3618-3626 (2009). | |
运输条件 | Room temperature in continental US; may vary elsewhere |
存放说明 | -20 |
纯度 | ≥98% |
计算分子量 | 435.6 |
分子式 | C26H45NO4 |
CAS号 | 120005-55-2 |
稳定性 | ≥ 1 year |
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