BX795

BX795 was initially developed as a PDK1 inhibitor (direct competitive inhibitor IC₅₀ = 11nM for PDK1) and has been shown to be a potent and relatively specific inhibitor of TBK1 and IKK-ε. It blocks the phosphorylation, nuclear translocation, and transcriptional activity of interferon regulatory factor 3. BX795 also is a potent inhibitor of cell growth of multiple cancer cell lines with IC₅₀ values ranging from submicromolar amounts (0.368 µM to greater than 450 µM).