IndraLab

Statements

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"Cotreatment of vorinostat with TPCA-1 (inhibitor of IKKβ that activates canonical NF-κB pathway) reduced NF-κB activity significantly (Figure 6F); however, MRT67307 (inhibitor of TBK1, which is a component of canonical STING pathway) cotreatment did not reduce vorinostat-induced NF-κB activity, illuminating the dominant effect of vorinostat on modulating NF-κB activity in PNET cells."
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"The IKKepsilon and TBK1 inhibitor MRT67307 inhibits CYLD phosphorylation independent of IKKepsilon and TBK1."
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"As it was shown previously that MRT67307 can inhibit IKKepsilon and TBK1 at concentrations as low as 1-2 muM, the concentration of 10 muM used may have led to off-target effects."
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"MRT67307 and BX795 efficiently inhibit TBK1 but are less potent in suppressing IKKε kinase activity ."
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"Taken together, these results indicate that MRT67307 inhibits the phospho (Ser418)-CYLD signal independent of its IKKepsilon and TBK1 inhibitory properties."
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"Here, we add to this information and show anti-schistosomula activities of other PAP-like compounds, such as CGP 60474 (inhibitor of cyclin-dependent kinase (CDK) and protein kinase C (PKC)), MRT67307 (inhibitor of IKK-ε and TBK1 and UKL1 and ULK2 [90]), 7070707105 (inhibitor of ALK5 and PKN3 kinase), AZ 191 (inhibitor of DYRK1B) and TAE684 (another inhibitor of ALK)."
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"MRT67307 specifically inhibits the IKKepsilon and TBK1 kinases, which are involved in controlling the production of Type1 interferons but also participate in a negative regulatory loop that restricts the extent of activation of the IKK complex [XREF_BIBR] [XREF_BIBR]."
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"However, originally developed as a ULK1/2 inhibitor [27], it turned out that the MRT67307 compound also inhibits TBK1 and IKKepsilon just as efficiently concerning kinase activities [28]."
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"In addition, the MRC PPU International Centre for Kinase Profiling reported in vitro specificity screens for several inhibitors (http://www.kinase-screen.mrc.ac.uk/kinase-inhibitors), showing that MRT67307 not only inhibits IKKepsilon and TBK1 and the AMPK related kinases MARK, MELK and NUAK, but also Mixed Lineage Kinase (MLK) 1 and MLK3, Janus kinase (JAK) 2, and Ca (2+)/calmodulin-dependent protein kinase kinase beta (CamKKbeta)."
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"For example, MRT67307, which is a new TBK1 inhibitor, derivatized from BX795, suppressed TBK1 activity with much higher specificity (IC 50 = 19nM), so that it did not inhibit other kinases such as JNK or p38 [XREF_BIBR]."
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"Blocking TBK1 and IKKepsilon during transduction of NK cells enabled their efficient transduction by VSV-G LVs as judged by YFPexpression of 40-50%, with half maximal effective concentrations of 1.1 microM (MRT67307), 5 microM (BX-795) and 24.8 microM (amlexanox)."
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