现货,Enzastaurin (LY317615) ,CAS号:170364-57-5,美国进口,TGF-beta / smad , PKC ,PKC 抑制剂和化合物,selleck,S1055

信号转导通路: TGF-beta / smad >> PKC >> PKC 抑制剂和化合物 >> Enzastaurin (LY317615)http://selleck.cn/enzastaurin-S1055.html

技术数据:

分子量(MW): 515.61

化学式:

C32H29N5O2

 

溶解度: DMSO ≥50mg/mL Water <1mg/mL Ethanol <1mg/mL

纯度: >99%

稳定性: at -20℃ 2 years

CAS号: 170364-57-5

生物活性

 

 

Enzastaurin (LY317615) induced marked dose-dependent growth inhibition in all MM cell lines investigated including MM.1S, MM.1R, RPMI 8226 (RPMI), RPMI-Dox40 (Dox40), NCI-H929, KMS-11, OPM-2, and U266.IC50 ranged from 0.6 to 1.6 μM. [1]

Enzastaurin has a direct effect on human tumor cells, inducing apoptosis and suppressing the proliferation of cultured tumor cells. Enzastaurin treatment also suppresses the phosphorylation of GSK3ßser9, ribosomal protein S6S240/244, and AKTThr308. [2]

Enz inhibited PKCβ and radiosensitized HDMEC with an enhancement ratio of 1.31 ± 0.05. Enz combined with RT reduced HDMEC capillary sprouting to a greater extent than either agent alone. Enz prevented radiation-induced GSK3β phosphorylation of serine 9 while having no direct effect on VEGFR phosphorylation. Treatment of xenografts with Enz and radiation produced greater reductions in microvessel density than either treatment alone. The reduction in microvessel density corresponded with increased tumor growth delay. [3]

 

 

 

 

 

参考文献

The Protein Kinase Cβ-Selective Inhibitor, Enzastaurin (LY317615.HCl), Suppresses Signaling through the AKT Pathway, Induces Apoptosis, and Suppresses Growth of Ann M. McNulty, Kimberly Ross Hanna, et al. Cancer Res 2005;65:7462-7469

Enzastaurin, an inhibitor of PKCβ, Enhances Antiangiogenic Effects and Cytotoxicity of Radiation against Endothelial Cells1,2 Aaron C. Spalding, Benjamin D. Zeitlin,et al. Translational Oncology 2008;1:195-201

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