BX795, originally described as a moderately potent inhibitor of PDK1 (IC50 = 111 nM)1, is, more importantly, a dual inhibitor of TBK1 and IKKepsilon (IC50s = 6 and 41 nM respectively)2. TBK1 and IKKepsilon regulate the production of Type I interferons during bacterial and viral infection via phosphorylation of the transcription factor IRF3. It also inhibited of MARK, MLK, NUAK, AurB, and ERK8.3 BX795 exhibited antitumor activity in human oral squamous cell carcinoma4, pancreatic ductal adenocarcinoma5, and Glioblastoma Multiforme6. BX795 has been used to enhance lentiviral transduction efficiency in human NK cells7-9 and human primary T cells10 for CAR-T cell therapy.
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