PF-543 (Synonyms: Sphingosine Kinase 1 Inhibitor II) PF-543 (Sphingosine Kinase 1 Inhibitor II) 是一种有效,选择性,可逆和鞘氨醇竞争性 SPHK1 抑制剂,IC50 为2 nM,Ki 为3.6 nM。PF-543 对 SPHK1 的选择性是 SPHK2 的 100 倍以上。PF-543 还是有效的全血中 1-磷酸鞘氨醇 (S1P) 形成的有效抑...
Pyne, S. Pyne, The sphingosine kinase 1 inhibitor 2-(p- hydroxyanilino)-4-(p-chlorophenyl)thiazole induces proteasomal degradation of sphingosine kinase 1 in mammalian cells. J. Biol. Chem. (2010) 285 38841-38852.Loveridge C, Tonelli F, Leclercq T et al (2010) The sphingosine kinase 1 ...
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et al. A selective sphingosine kinase 1 inhibitor integrates multiple molecular therapeutic targets in human leukaemia. Blood 112, 1382–1391 (2008). This paper identifiedthe first SK1-selective inhibitor. Article CAS PubMed PubMed Central Google Scholar Kapitonov, D. et al. Targeting sphingosine...
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Furthermore, oncogenic K-Ras altered SL metabolism, with an increase of long-chain (LC) C18, C20 ceramides (Cer), and very-long-chain (VLC) C22:1, C24 Cer, and an increase of sphingosine kinase 1 (SK1) expression. Since Cer and sphingosine-1-phosphate have been shown to exert ...
Sphingosine kinase 1 (SphK1) is over-expressed in many cancers and therefore serves as a biomarker for cancer prognosis. SKI-5C is a new SphK1 inhibitor, and until now its molecular function in Wilms’ tumor cells remained unknown. Here, using CCK-8 and nude mice experiments we assessed ...
We used a potent inhibitor of sphingosine kinase to study its effect on colony formation and cell growth in GBM cells with a limited dilution and WST assay. Moreover, cell death was determined by measuring caspase-3 activity using flow cytometry. RESULTS: A sphingosine kinase inhibitor reduced ...
Sphingosine-1-phospate is a potent bioactive lipid metabolite that regulates cancer progression. Because sphingosine kinase 1 and sphingosine kinase 2 (SPHK 1/2) are both essential for sphingosine-1-phospate production, they could be a therapeutic target in various cancers. Peretinoin, an acyclic...
K145, a sphingosine kinase 2 inhibitor, inhibits solitary plasmacytoma cell growthSolitary plasmacytoma (SP) is a rare disease. It is characterized by a localized proliferation of neoplastic monoclonal plasma cells either in the bone (solitary bone plasmacytoma, SBP) or in soft tissue (solitary ...