SKI-178
SKI-178(SKI-178)
CAS: 1259484-97-3
化学式: C21H22N4O4
| 中文名 | SKI-178 |
| 英文名 | SKI-178 |
| 别名 | 化合物SKI-178 |
| 英文别名 | SKI-178 SKI 178 N'-(1-(3,4-Dimethoxyphenyl)ethylidene)-3-(4-methoxyphenyl)-1H-pyrazole-5-carbohydrazide |
| CAS | 1259484-97-3 |
| 化学式 | C21H22N4O4 |
| 分子量 | 394.42 |
| 溶解度 | 溶于DMSO |
| 存储条件 | -20℃ |
| 产品用途 | SKI-178 is a sphingosine kinase 1 (SphK1) inhibitor (IC50 = 0.1-1.8 μM). SKI-178 induces prolonged mitosis followed by apoptotic cell death through the intrinsic apoptotic cascade. The sustained activation of CDK1 during prolonged mitosis, mediated by SKI-178 leads to the simultaneous phosphorylation of the prosurvival Bcl-2 family members, Bcl-2 and Bcl-xl, as well as the phosphorylation and subsequent degradation of Mcl-1. SKI-178 is a novel therapeutic agent for the treatment of AML, including multidrug-resistant/recurrent AML subtypes. |
| 参考资料 展开查看 | 1: LeBlanc FR, Liu X, Hengst J, Fox T, Calvert V, Petricoin EF 3rd, Yun J, FeithDJ, Loughran TP Jr. Sphingosine kinase inhibitors decrease viability and inducecell death in natural killer-large granular lymphocyte leukemia. Cancer BiolTher. 2015;16(12):1830-40. doi: 10.1080/15384047.2015.1078949. PubMed PMID:26252351; PubMed Central PMCID: PMC4847818. 2: Dick TE, Hengst JA, Fox TE, Colledge AL, Kale VP, Sung SS, Sharma A, Amin S,Loughran TP Jr, Kester M, Wang HG, Yun JK. The apoptotic mechanism of action ofthe sphingosine kinase 1 selective inhibitor SKI-178 in human acute myeloidleukemia cell lines. J Pharmacol Exp Ther. 2015 Mar;352(3):494-508. doi:10.1124/jpet.114.219659. Epub 2015 Jan 6. PubMed PMID: 25563902; PubMed CentralPMCID: PMC4352591. 3: Hengst JA, Wang X, Sk UH, Sharma AK, Amin S, Yun JK. Development of asphingosine kinase 1 specific small-molecule inhibitor. Bioorg Med Chem Lett.2010 Dec 15;20(24):7498-502. doi: 10.1016/j.bmcl.2010.10.005. Epub 2010 Nov 1.PubMed PMID: 21050755. |
SKI-178 - 配置溶液浓度参考
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.535 ml | 12.677 ml | 25.355 ml |
| 5 mM | 0.507 ml | 2.535 ml | 5.071 ml |
| 10 mM | 0.254 ml | 1.268 ml | 2.535 ml |
| 5 mM | 0.051 ml | 0.254 ml | 0.507 ml |
最后更新：2024-01-02 23:10:35
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