BX795

BX795 is a potent, ATP-competitive small molecule inhibitor that targets 3-phosphoinositide-dependent protein kinase 1 (PDPK1) and the IKK-related kinases, TANK-binding kinase 1 (TBK1) and I-kappa-B kinase epsilon (IKKε). Originally developed by Berlex Biosciences to inhibit the PDK1/Akt pathway, it was subsequently found to be a highly effective inhibitor of the innate immune response by blocking the phosphorylation of IRF3 and the subsequent production of Type I interferons. In the context of oncology, BX795 is frequently used as a tool compound to investigate synthetic lethal interactions, such as the combined inhibition of PDPK1 and BRAF in BRAF-mutant anaplastic thyroid cancer. Its mechanism involves inducing DNA damage, G2/M cell cycle arrest, and mitochondrial-mediated apoptosis through the generation of reactive oxygen species (ROS).

Other names

N-(3-(5-bromo-2-(2-(pyridin-2-ylamino)ethylamino)pyrimidin-4-ylamino)phenyl)propionamide