IndraLab

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"We have shown here that TBK1 inhibition by BX795 leads to increased mitochondrial biogenesis in both the WT and glaucomatous (E50K) hRGCs."
36828933
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"Knockdown or BX795 inhibition of TBK1 effectively controlled the proliferation and migration of bladder cancer cells by attenuating AKT phosphorylation [129]."
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"Interestingly BX795, a molecule which inhibits TBK1 and IKKepsilon, has recently been shown to inhibit IFN-I production and signaling in human PBMCs with a mutation induced interferonopathy [8]."
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"Treatment with 5 muM BX795 (a pharmacological inhibitor of TBK1, also blocker of IFN-beta) and siTBK1 increased the bacterial load of intracellular M. bovis in both J774a.1 and BMDM macrophages after 24 and 48 h of infection."
30042930
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"To determine if these kinases are involved in the ability of C5a and C3a to suppress IFN-beta production, we used CGI-1746 to inhibit BTK, Wortmannin to inhibit PI3K and Akt, U0126 to inhibit Erk, BX795 to inhibit TBK1, and SB202190 to inhibit p38 MAPK."
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"As such, we carried out a series of experiments by using BX795 that potently inhibits TBK1 activity XREF_BIBR."
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"We find that inhibition of TBK1 activity either by the semi-selective TBK1 and IKKepsilon inhibitor BX795 or by siRNA mediated knockdown abrogates HMPV induced expression of IRF1."
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"MuV induced p-p65 and p-IRF3 levels in Sertoli cells were evidently reduced by a 2-h pretreatment of cells with BAY11-7082 (inhibitor of IkappaBalpha degradation) and BX795 (inhibitor of TBK1), respectively (XREF_FIG, left panels)."
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"XREF_BIBR BX795 blocks the catalytic activity of TBK1 and IKKepsilon (IKBKE) kinases by impeding their phosphorylation and therefore may affect signaling downstream of several innate pattern recognition receptors."
33665226
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"Although initially developed as a PDK1 inhibitor, recent studies have found that BX795 can also inhibit TANK binding kinase-1 (TBK1) and closely related IkappaB kinase epsilon (IKKepsilon)."
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"Firstly, BX795, which can also inhibit TBK1, PDK1, p38 and JNK resulted in a significant reduction in PSA mRNA and protein levels and also reduced AR levels consistent with the CAY10576 data (XREF_SUPPLEMENTARY)."
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"BAY11-7082 inhibits NF-κB expression by blocking IκBα phosphorylation, while BX795 inhibits IRF3 activation by blocking the catalytic activities of Tank-binding kinase 1 (TBK1) and IκB kinase ε (IKKε) (37)."
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"Chemical inhibition of HSP90 (by 17-DMAG) or of TBK1 (by BX795) decreased ISD stimulated Ifnb1 and CXCL10 production in mouse lung fibroblasts and human MoDCs, similar to the reductions in these cytokines caused by CDC37 inhibition (XREF_FIG and XREF_SUPPLEMENTARY)."
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"Finally, a small molecule inhibitor of TANKbinding kinase 1 (TBK1), BX795, suppresses HSV viral protein synthesis with antiviral activity on par with trifluridine in animal models of ocular HSV infection."
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"BX795 was originally identified as an inhibitor of 3-phosphoinositide-dependent protein kinase (PDK1) but has been shown to inhibit TBK1 and IKKε to an even greater degree ( Bain et al., 2007; Feldman[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"The TUNEL assay ( Fig. 2 C) and Comet assay ( Fig. 2 D) further confirmed DNA fragmentation induced by BX795.Since BX795 is an inhibitor of TBK1 ( Bain et al., 2007 ), we checked the protein expressio[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"OV-90 cells were pre-treated with 10 μM BX795 (a small molecule inhibitor of TBK1/IKKε ( Li et al., 2020 )) for 2 h followed by transfection with reovirus dsRNA for 24 h."
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"However, such activation for AMPKα (Fig. 4e, g) and PGC1α (Fig. 4e, i) were not observed for the E50K hRGCs under BX795 mediated TBK1 inhibition."
36828933
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"The compound BX795 was developed as an inhibitor of the kinase PDK1 and was later discovered to potently inhibit TBK1."
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"Moreover, GM-DCs in which TBK1 and IKKepsilon were inhibited by BX795 showed substantial impairment in the phosphorylation of Akt at Ser473 and Thr308 and of PRAS40 and the ribosomal protein S6, and this was more profound than the inhibition observed after inhibition of PI (3) K or mTOR (XREF_FIG and XREF_SUPPLEMENTARY)."
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"In particular, BX795 (a specific inhibitor of TBK1) significantly inhibited poly(I:C)-induced antiviral responses in WT granulosa cells and completely abolished responses in TLR3 –/– cells."
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"MRT67307 and BX795 efficiently inhibit TBK1 but are less potent in suppressing IKKε kinase activity ."
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"However, TBK1 inhibition by BX795 showed a robust increase in mitochondrial mass at early and longer treatments for the WT and during longer treatments (18 h, 24 h) for E50K hRGCs (Fig. 4a, b)."
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"In vitro, BX795 can also inhibit TBK1, PDK1, Aurora B, MARK1, MARK2, MARK4, NUAK1, MLK1, MLK2, MLK3 with the range of 5-111 nM [XREF_BIBR]."
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"Additionally, the expression of TBK1 (a kinase downstream of cGAS/STING pathway and ZBP1), IRF3, and activated TBK1 are increased in the PBMCs of Sjögren’s syndrome patients, and treatment with BX795 [MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"BX795 is an inhibitor of TBK1 and can also inhibit 3-phosphoinositide-dependent kinase 1 (PDK1)."
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"We next tested if TBK1 inhibition by BX795 provoked mitotic defects or spindle abnormalities."
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"These data together support further exploration of the potential of TBK1 inhibitors as treatment for IFNpos systemic autoimmune diseases.A limitation of this study is that BX795 inhibits not only TBK1[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"TBK1 inhibition by BX795 increases the sensitivity of breast cancer cells to tamoxifen treatment (33) and has an antiproliferative effect in human oral squamous cell carcinoma (34)."
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"BX795 also inhibits TBK1 enhancement of bladder cancer cell proliferation and migration (35)."
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"This ionizing radiation-induced T228 phosphorylation was dose dependent ( Figures 2 D and S2 F) and could be blocked by shRNA-mediated TBK1 depletion ( Figures 2 F and S2 G), BX795-mediated TBK1 inhib[MISSING/INVALID CREDENTIALS: limited to 200 char for Elsevier]"
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"Inhibition of TBK1 by BX795 or knockdown of TBK1 by shTBK1 lentivirus blocked the capacity of MVNP to up-regulate IL6 gene expression in both NIH3T3 cells and primary BMM, as well as blocked the MVNP induced increase in osteoclast numbers after RANKL or TNF-alpha stimulation."
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"To inhibit TBK1, cells were treated with 0.5 muM BX795 (Axon Medchem or Tocris Bioscience)."
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"We estimate that CCT128930 inhibits only pS6 (and not pRAS40 and pAKT), and that BX795 inhibits the mTOR pathway rather than TBK1, at concentrations of 3.33 and 10 muM."
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