tcsc0259 BX795

BX795 is a potent and selective dual inhibitor of TBK1/PDK1 with IC₅₀s of 2 nM/6 nM, respectively, and has > 50 fold selectivity over PKA, PKC, c-Kit, GSK3β etc.

IC50 & Target: IC50: 2 nM (TBK1), 6 nM (PDK1)

In Vitro: BX795 effectively blocks PDK1 activity in PC-3 cells, as shown by their ability to block phosphorylation of S6K1, Akt, PKCδ, and GSK3β. BX795 potently inhibits tumor cell growth on plastic with IC₅₀ of 1.6, 1.4, and 1.9 μM for MDA-468, HCT-116 and MiaPaca cells, respectively. In soft agar, BX795 displays higher growth inhibition with IC₅₀ of 0.72, and 0.25 μM for MDA-468, and PC-3 cells, respectively^[1]. In addition, BX795, as an inhibitor of the TBK1/IKKε, blocks TBK1- and IKKε-mediated activation of IRF3 and production of IFN-β^[2]. In platelet physiological responses, BX795 produces inhibitory effect on 2-MeSADP-induced or collagen-induced aggregation, ATP secretion and thromboxane generation^[3].