IndraLab

Statements

Amlexanox inhibits IKBKE. 14 / 15
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"Amlexanox Amlexanox is an inhibitor of noncanonical IkappaB kinases IKK-epsilon and TANK binding kinase 1."
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"Recently, Reilly et al. [XREF_BIBR] discovered a small molecule inhibitor of IKKepsilon and TBK1 kinases called amlexanox, which has been shown to selectively inhibit both IKKepsilon and TBK1."
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"Consistent with this view , global knockout of the cGAS-cGAMP-STING downstream target TBK1 ( 37 ) or IRF3 ( 38 ) , or pharmacological inhibition of IkappaB kinase epsilon ( IKKepsilon ) and TBK1 by amlexanox , reduced body weight , enhanced insulin sensitivity , and improved glucose tolerance in obese mice and in a subset of patients with type 2 diabetes ( 34,39 ) ."
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"Recently, amlexanox has been shown to inhibit TBK1 and IKKepsilon, both of which are induced in the liver and fat by high-fat diet mediated NF-kappaB activation [XREF_BIBR]."
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"As more effective therapeutic strategies are urgently needed for treating hepatic fibrosis and cirrhosis , inhibition of TBK1 and IKKepsilon by amlexanox may be a promising therapeutic strategy to cure fibrosis , which could allow for remodelling and regression of fibrosis ."
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"Based on histopathologic analysis using H & E and Sirius-red staining , inhibition of TBK1 and IKKepsilon by amlexanox markedly reduced biliary hyperplasia and collagen deposition in the livers of mice fed with DDC diet ( Figure 2B , C ) ."
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"Amlexanox, which is known to inhibit TBK1 and IKKepsilon selectively, is an approved drug for the treatment of bronchial asthma, allergic rhinitis, and conjunctivitis in Japan and elsewhere."
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"Amlexanox Enhances Temozolomide-Induced Antitumor Effects in Human Glioblastoma Cells by Inhibiting IKBKE and the Akt-mTOR Signaling Pathway."
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"Amlexanox is a specific inhibitor of IKKepsilon and TBK1."
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"14 We found that amlexanox treatment could inhibit the IKBKE protein and alter the abundance and phosphorylation status of the Hippo pathway proteins in glioma cells."
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"Collectively, these studies show that IKBKE plays a pivotal role in human malignancy and could be a critical therapeutic target for PDAC.Recent studies have identified two small-molecule compounds, amlexanox and CYT387, which directly inhibit IKBKE/TBK1 kinase activity [10,18,19]."
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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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"Collectively , we found that inhibition of the TBK1 and IKKepsilon by amlexanox is a promising therapeutic strategy to cure liver fibrosis ."
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"Amlexanox blocks activity of TBK1 and IKKepsilon with a half maximal inhibitory concentration (IC50) of approximately 1-2 muM."
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