货号 | 18624-10mg |
描述 | Safingol is the L-threo diastereomer of D-erythro-sphinganine (Item No. 10007945) Both forms of sphinganine inhibit PKC by binding at the regulatory phorbol-binding domain (IC50s = 7 and 24 µM for erythro-sphinganine and safingol, respectively).1,2 Safingol also inhibits sphingosine kinases (Ki = 3-5 µM).3,4,5 Safingol, alone or in combination with chemotherapeutic agents, is cytotoxic against cancer cell lines.3,6 |
别名 | L-threo-Dihydrosphingosine;L-threo-Sphinganine; |
供应商 | Cayman |
应用文献 | |
1.Hannun, Y.A.,Loomis, C.R.,Merrill, A.H., Jr., et al. Sphingosine inhibition of protein kinase C activity and a phorbol dibutyrate binding in vitro and in human platelets. The Journal of Biological Chemisty 261(27), 12604-12609 (1986). 2.Wilson, E.,Olcott, M.C.,Bell, R.M., et al. Inhibition of the oxidative burst in human neutrophils by sphingoid long-chain bases. Role of protein kinase C in activation of the burst. The Journal of Biological Chemisty 261(27), 12616-12623 (1986). 3.Kim, J.W.,Kim, Y.W.,Inagaki, Y., et al. Synthesis and evaluation of sphingoid analogs as inhibitors of sphingosine kinase. Bioorganic & Medicinal Chemistry 13, 3475-3485 (2005). 4.Baek, D.J.,Macritchie, N.,Anthony, N.G., et al. Structure-activity relationships and molecular modeling of sphingosine kinase inhibitors. Journal of Medicinal Chemistry 56(22), 9310-9327 (2013). 5.Plano, D.,Amin, S., and Sharma, A.K. Importance of sphingosine kinase (SphK) as a target in developing cancer therapeutics and recent developments in the synthesis of novel SphK inhibitors. Journal of Medicinal Chemistry 57(13), 5509-5524 (2014). 6.Matula, K.,Collie-Dugid, E.,Murray, G., et al. Regulation of cellular sphingosine-1-phosphate by sphingosine kinase 1 and sphingosine-1-phopshate lyase determines chemotherapy resistance in gastroesophageal cancer. BMC Cancer 15:762, (2015). | |
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 | 301.5 |
分子式 | C18H39NO2 |
CAS号 | 15639-50-6 |
稳定性 | ≥ 1 year |
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