Purity ~95% (HPLC). A cell-permeable BX795 analog that acts as a potent, ATP-competitive, and reversible dual kinase inhibitor of TBK1/IKK epsilon (IC50 = 19 and 160nM, respectively) with excellent selectivity over IKKalpha and IKKbeta (IC50 > 10uM). 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 41nM, respectively), SIK2 (IC50 = 67nM) and Aurora B, JAK2, and MLK1,3 (> than 90% inhibition at 1uM) in a 108-kinase panel. Increases TNF-alpha-stimulated NF-kB-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 res
Size
5mg
Concentration
n/a
Applications
n/a
Other Names
IKK epsilon/TBK1 Inhibitor II, MRT67307 (TANK Binding Kinase 1/IKKinducible Inhibitor II, N-(3-(5-Cyclopropyl-2-(3-(morpholinomethyl)phenylamino)pyrimidin-4-ylamino)propyl)cyclobutanecarboxamide)