BX 795 was initially developed as a PDK1 inhibitor. Recent study highlighted on its bioactivitiy as a potent and relatively specific inhibitor of TBK1 and closely related IKKε, with IC50 values to be 6, 41, and 111 nM for TBK1, IKKε and PDK1 respectively.
References:
R I Feldman et al. Novel Small Molecule Inhibitors of 3-Phosphoinositide-dependent Kinase-1. J. Biol. Chem., 2005, 280, 20, 19867-19874. [online]
J Bain et al. The selectivity of protein kinase inhibitors: a further update. Biochem. J. 2007, 408, 297–315.[online Abstract]
C Peifer, D R. Alessi, Small-Molecule Inhibitors of PDK1. ChemMedChem. 2008, 3 (10), Review. [online abstract]
K Clark 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 phosphoylation and activation. J. Biol. Chem. 2009, 284, 14136-14146. [online]
Chemical Name: Pyrrolidine-1-carboxylic acid [3-(5-iodo-4-{3-[(thiophene-2-carbonyl)-amino]-propylamino}-pyrimidin-2-ylamino)-phenyl]-amide
