TBK1/IKKε inhibitor

TBK1/IKKε signaling inhibition by MRT67307

MRT67307 is a potent, reversible kinase inhibitor specifically blocking the function of TBK1 (TANK-binding kinase 1) and I-kappa-B kinase (IKK) epsilon (IKKε, or IKBKE), thereby preventing the phosphorylation of IRF3 (interferon regulatory factor 3) and subsequent expression of interferon-stimulated genes (ISGs) [1]. Unlike BX795 from which it is derived, MRT67307 has no noted effect on the canonical IKKs, IKKα, or IKKβ, that are involved in the activation of NF-κB [1]. Additionally, MRT67307 is a highly potent inhibitor of ULK1, a key component of the autophagy pathway [2].

Key features:

MRT67307 potently inhibits IRF signaling in a dose-dependent manner.
MRT67307 does not affect NF-κB signaling.
InvitroFit™ grade: each lot is highly pure (≥95%) and functionally tested.

References:

1. Clark, K. et al., 2011. Novel cross-talk within the IKK family controls innate immunity. Biochem J 434, 93-104.
2. Petherick, K.J. et al., 2015. Pharmacological inhibition of ULK1 kinase blocks mammalian target of rapamycin (mTOR)-dependent autophagy. J Biol Chem 290, 11376-11383.

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