Cat. No. 4318
Chemical Name: N-[3-[[5-Iodo-4-[[3-[(2-thienylcarbonyl)amino]propyl]amino]-2-pyrimidinyl]amino]phenyl]-1-pyrrolidinecarboxamide
Biological ActivityInhibitor of 3-phosphoinositide-dependent kinase 1 (PDK1). Inhibits Akt phosphorylation at Thr308 in PC3 cells; also inhibits anchorage-independent growth of PC3 and MDA-MB-468 cells. Exhibits activity at other kinases, including TANK-binding kinase 1 (TBK1), Aurora B and IκB kinase ε (IKKε).
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
Feldman et al (2005) Novel small molecule inhibitors of 3-phosphoinositide-dependent kinase-1. J.Biol.Chem. 280 19867. PMID: 15772071.
Tamguney et al (2008) Analysis of 3-phosphoinositide-dependent kinase-1 signaling and function in ES cells. Exp.Cell Res. 314 2299. PMID: 18514190.
Clark et al (2009) 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. J.Biol.Chem. 284 14136. PMID: 19307177.
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Keywords: BX 795, supplier, BX795, pdk1, inhibitors, 3-phosphoinositide-dependent, kinase-1, TBK1, TANK-binding, kinase, 1, Aurora, B, IkBe, IkappaBepsilon, IκBε, kinase, multi-kinase
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