IndraLab

Statements

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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 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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"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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"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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"The compound BX795 was developed as an inhibitor of the kinase PDK1 and was later discovered to potently inhibit TBK1."
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No evidence text available
Other
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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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"Moreover, TBK1 and AKT, transforming growth factor activated kinase (TAK)-1/c-Jun N-terminal kinase (JNK)/mitogen-activated protein kinase kinase 4 (MKK4) for AP-1 activation, and Janus kinase 2 (JAK2)/STAT1 were inhibited by BX795."
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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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"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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"To inhibit TBK1, cells were treated with 0.5 muM BX795 (Axon Medchem or Tocris Bioscience)."
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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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"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."
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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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"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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"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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"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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"We next tested if TBK1 inhibition by BX795 provoked mitotic defects or spindle abnormalities."
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No evidence text available
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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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"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."
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"BX795 is an inhibitor of TBK1 and can also inhibit 3-phosphoinositide-dependent kinase 1 (PDK1)."
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"BX795 [originally developed as a 3phosphoinositidedependent protein kinase 1 (PDK1)] [90] and a series of azabenzimidazole derivatives [91] inhibit both IKKe and TBK1 at low nanomolar concentrations [92] ."
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