MRT67307 hydrochloride

Packaged under inert gas

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Cell permeable: yes

Primary Target
TBK1 kinase dimer interface

Reversible: yes

Secondary Target
IKKe, MARK, SIK

Toxicity: Standard Handling (A)

A cell-permeable BX795 analog (>Cat. No. 204001) that acts as a potent, ATP-competitive, and reversible dual kinase inhibitor of TBK1/IKKε (IC₅₀ = 19 and 160 nM, respectively) with excellent selectivity over IKKα and IKKβ (IC₅₀ >10 µM). Interacts with the TBK1 kinase dimer interface and stabilizes the inactive DFG-out conformation. Also blocks the activity of MARK (microtubule- associated protein (MAP)-microtubule affinity regulating kinase) 1, 2, 3, and 4 (IC₅₀ = 27, 52, 36, and 41 nM, respectively), SIK2 (IC₅₀ = 67 nM) and Aurora B, JAK2, and MLK1,3 (> than 90% inhibition at 1 µM) in a 108-kinase panel. Increases TNF-α-stimulated NF-κB-dependent gene transcription in wild-type macrophages and enhances CREB-dependent gene transcription by promoting dephosphorylation of CREB-regulated transcription coactivator (CRTC3). Shown to aid TLR-stimulated production of anti-Inflammatory cytokines in macrophages while suppressing the secretion of pro-inflammatory cytokines. In response to pro-inflammatory stimuli, pre-treatment of BX795 robustly suppresses the activation of JNK and p38α, whereas MRT67307 does not exhibit such off-target effects.

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water and salt.

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