TBK1/IKKε inhibitor

TBK1/IKKε signaling inhibition by BX795

BX795 is a potent inhibitor of the noncanonical IkB kinases TANK-binding kinase 1 (TBK1) and IkappaB kinase-epsilon (IKKε) [1]. TBK1 and IKKε play a central role in the innate immune response. Notably, these noncanonical IkappaB kinase homologs are essential components of the interferon regulatory factor (IRF) signaling pathway.

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Mode of action:

BX795 inhibits the catalytic activity of TBK1/IKKε by blocking their phosphorylation. BX795, an aminopyrimidine compound, was developed as an inhibitor of 3-phosphoinositide-dependent kinase 1 (PDK1) [1].

Studies have demonstrated that BX795 is a potent inhibitor of the IKK-related kinases, TANK-binding kinase 1 (TBK1), and IKKε, and hence of IRF3 activation and IFN-β production [2, 3].

Key features:

A potent inhibitor of TBK1 and IKK-ε
InvitroFit™ grade: each lot is highly pure (≥95%) and functionally tested

References:

1. Feldman RL. et al., 2005. Novel Small Molecule Inhibitors of 3-Phosphoinositide- dependent Kinase-1. J. Biol. Chem., 280: 19867 - 19874.
2. Clark K. et al., 2009. Use of the Pharmacological Inhibitor BX795 to Study the Regulation and Physiological Roles of TBK1 and I{kappa}B Kinase {epsilon}: a distinct upstream kinase mediates Ser-172 phosphorylation and activation. J. Biol. Chem., 284: 14136 - 14146.
3. Bain J. et al., 2007. The selectivity of protein kinase inhibitors: a further update, 408: 297-315.

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2 Search results: TLRL-BX7-2