应用 |
Human cisplatin-resistant gastric cancer cell line was treated with SKI-II to study the mechanism of reversion of multidrug resistance. |
产品介绍 |
SKI II是一种合成的鞘氨醇激酶 (SK) 抑制剂, 抑制SK1和SK2, IC50值分别为78 μM和45 μM。 |
备注 |
SKI II is a highly selective and non ATP-competitive S1P receptor inhibitor with IC50 of 0.5 μM, while exhibits no inhibitory on other kinases including PI3K, PKCα and ERK2. |
生化机理 |
SKI II is a selective non-lipid inhibitor of SphK(sphingosine kinase) (IC50 = 0.5 μM); does not act at ATP-binding site. SKI II displays no inhibition of ERK2, PI 3-kinase, or PKCα at concentrations up to 60 μM. Reduces levels of sphingosine-1-phosphate in MDA-MB-231 breast cancer cells. SKI II induces apoptosis and inhibits prpliferation in several other tumor cell lines in vitro (IC50 = 0.9-4.6 μM). |
别名 |
SKI-II;4-[[4-(4-氯苯基)-2-噻唑基]氨基]苯酚;Sphingosine Kinase Inhibitor 2;4-[[4-(4-Chlorophenyl)-2-thiazolyl]amino]phenol |