| 货号 | 14932-50mg |
| 描述 | 3-Phosphoinositide-dependent protein kinase 1 (PDK1) is a serine-threonine kinase that phosphorylates and activates a range of other kinases, including PKB, PKA, and certain isoforms of PKC.1 BX-795 is a potent, ATP-competitive inhibitor of PDK1 in vitro(IC50 = 11 nM) and in cells (IC50 = 300 nM).2 At comparable concentrations, BX-795 also inhibits ERK8, MAPK-interacting kinase 2, Aurora B, Aurora C, MAP/microtubule affinity-regulating kinases 1-4, TNF receptor associated factor-associated NF-κB activator-binding kinase 1, IκB kinase ε, and additional kinases.3,4,5 |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Peifer, C. and Alessi, D.R. Small-molecule inhibitors of PDK1. ChemMedChem 3(12), 1810-1838 (2008). 2.Feldman, R.I.,Wu, J.M.,Polokoff, M.A., et al. Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. The Journal of Biological Chemisty 280(20), 19867-19874 (2005). 3.Bain, J.,Plater, L.,Elliot, M., et al. The selectivity of protein kinase inhibitors: A further update. Biochemistry Journal 408, 297-315 (2007). 4.Tamgüney, T.,Zhang, C.,Fiedler, D., et al. Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cells. Experimental Cell Research 314(11-12), 2299-2312 (2008). 5.Clark, K.,Plater, L.,Peggie, M., et al. Use of the pharmacological inhibitor BX795 to study the regulation and physiological roles of TBK1 and IκB kinase ε: A distinct upstream kinase mediates Ser-172 phosphorylation and activation. The Journal of Biological Chemisty 284(21), 14136-14146 (2009). | |
| 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 | 591.5 |
| 分子式 | C23H26IN7O2S |
| CAS号 | 702675-74-9 |
| 稳定性 | ≥ 2 years |
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