Key Specifications Table
Pricing & Availability
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|5.06306.0001||Glass bottle||5 mg||
|Overview||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.
|Synonyms||TANK Binding Kinase 1/IKKinducible Inhibitor II, N-(3-(5-Cyclopropyl-2-(3-(morpholinomethyl)phenylamino)pyrimidin-4-ylamino)propyl)cyclobutanecarboxamide|
|Structure formula Image|
|Primary Target||TBK1 kinase dimer interface|
|Secondary target||IKKe, MARK, SIK|
|Purity||≥95% by HPLC|
|Safety Information according to GHS|
|Product Usage Statements|
|Packaged under inert gas||Packaged under inert gas|
IKKε/TBK1 Inhibitor II, MRT67307 - CAS 1190378-57-4 - Calbiochem SDS
|Bruni, D., et al. 2013. J. Immunol. 190, 2844.
Tu, D., et al. Cell Reports 3, 747.
Larabi, A., et al. Cell Reports 3, 734.
Clark, K., et al. 2012. Proc. Natl. Acad. Sci. USA 109, 16986.
Clark, K., et al. 2011. Proc. Natl. Acad. Sci. USA 108, 17093.
Clark, K., et al. 2011. Biochem. J. 434, 93.
Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.