| 货号 | 16726-1mg |
| 描述 | Sotrastaurin is a protein kinase C (PKC) inhibitor that displays immunosuppressive activity, blocking T cell activation through the disruption of downstream NF-κB signaling.1,2 In cell-free assays, sotrastaurin was reported to inhibit PKCα, βI, δ, ε, η, and θ with Ki values of 0.95, 0.64, 2.1, 3.2, 1.8, and 0.22 nM, respectively.1 Sotrastaurin can prevent the production of various cytokines by activated T cells, macrophages, and keratinocytes in vitro and has been shown to inhibit an acute allergic contact dermatitis response in rats when dosed orally at 30 mg.3 However, clinical investigation of sotrastaurin for its potential to prevent renal transplant rejection was halted during phase II testing due to high incidence of rejection.4 Sotrastaurin is also reported to activate Wnt/β-catenin signaling via the inhibition of glycogen synthase kinase 3 (IC50s = 229 and 172 nM for α and β isoforms, respectively), which is essential for embryogenesis and adult stem cell maintenance.5,6 |
| 别名 | AEB071; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Evenou, J.P.,Wagner, J.,Zenke, G., et al. The potent protein kinase C-selective inhibitor AEB071 (sotrastaurin) represents a new class of immunosuppressive agents affecting early T-cell activation. Journal of Pharmacology and Experimental Therapeutics 330(3), 792-801 (2009). 2.Vafadari, R.,Kraaijeveld, R.,Weimar, W., et al. Tacrolimus inhibits NF-κB activation in peripheral human T cells. PLoS One 8(4), 1-9 (2014). 3.Skvara, H.,Dawid, M.,Kleyn, E., et al. The PKC inhibitor AEB071 may be a therapeutic option for psoriasis. Journal of Clinical Investigation 118(9), 3151-3159 (2008). 4.Hardinger, K.L. and Brennan, D.C. Novel immunosuppressive agents in kidney transplantation. World J.Transplant. 3(4), 68-77 (2013). 5.Verkaar, F.,Blankesteijn, W.M.,Smits, J.F.M., et al. β-Galactosidase enzyme fragment complementation for the measurement of Wnt/β-catenin signaling. The FASEB Journal 24(4), 1205-1217 (2010). 6.Verkaar, F.,van der Stelt, M.,Blankesteijn, W.M., et al. Discovery of novel small molecule activators of β-catenin signaling. PLoS One 6(4), 1-7 (2011). | |
| 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 | 438.5 |
| 分子式 | C25H22N6O2 |
| CAS号 | 425637-18-9 |
| 稳定性 | ≥ 2 years |
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