BX-795 is an aminopyrimidine-based, ATP-competitive inhibitor of PDK1, TBK1, and IKKe, with IC50 values of 11 nM, 6 nM, and 41 nM, respectively. [1, 2] BX-795 also potently inhibits ERK8, MNK2, Aurora B, Aurora C, and MARK3. [3] BX-795 inhibits both Thr308-Akt and Thr389-S6K1 phosphorylation at an IC50 of 300 nM. [2]

BX-795 has proven to be a powerful tool in the elucidation of TBK1's and IKKe's role in autophosphorylation events. [1] In particular, it wasfound that BX-795 blocked the autophosphorylation of overexpressed TBK1 and IKKe at Ser172, but did not inhibit endogenous TBK1 and IKKe in response to LPS, poly (I:C), IL-1a). These observations demonstrate that the phosphorylation of Ser172 and activation of TBK1 and IKKe are catalyzed by a distince protein kinase in vivo and that TBK1 and IKKe control a feedback loop that limits their activation to prevent hyperactivation by these enzymes. [1]