IndraLab

Statements

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"Consistent with a previous report xref , IKK2 inhibition by TPCA-1 did not cause ARPE-19 cell death even with TNFα induction ( xref )."
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"To test this hypothesis, arrested cells were maintained for 3 days in the presence or absence of the anti-inflammatory compound TPCA-1, which blocks NF-κB activation by inhibiting the upstream kinase IKK2 ."
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"Although BMS and TPCA-1 are specific inhibitors of IKKbeta, they may have non target effects on TM expression."
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"Pharmacological inhibition of IKKβ by TPCA-1 or PF184 reduced p50 nuclear translocation and A3A up-regulation in PC9 and MGH064–1 cells in presence of TKI ( xref , xref )."
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"Our results suggest that IKK2 inhibition by its specific inhibitor TPCA-1 is able to block laser induced CNV through the IKK-NF-kappaB signaling pathway, and in turn, the transcription of its downstream target genes that promote neovascularization."
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"To determine the role of NF-κB, we evaluated the effect of TPCA-1, which suppresses NF-κB by selectively inhibiting IKK-2 (41, 42)."
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"Consistent with a previous report XREF_BIBR, IKK2 inhibition by TPCA-1 did not cause ARPE-19 cell death even with TNFalpha induction (XREF_FIG)."
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"TPCA-1 is a selective inhibitor of human IkappaB kinase-2 (IKK-2) that inhibits production of pro inflammatory cytokines in vitro and in vivo and inhibits NF-kappaB nuclear localization XREF_BIBR, XREF_BIBR, XREF_BIBR."
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"Our results suggest that IKK2 inhibition by its specific inhibitor TPCA-1 is able to block laser-induced CNV through the IKK-NF-κB signaling pathway, and in turn, the transcription of its downstream target genes that promote neovascularization."
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"As for drug sensitivity analysis, SFXN4 was predicted to be responsive to Vorinostat (an inhibitor targeting HDAC 1, HDAC2, HDAC3, HDAC6, HDAC7, and HDAC11), Methotrexate (adihydrofolate reductase inhibitor), 5-Fluorouracil (athymidylate synthase inhibitor) and TPCA-1 (an inhibitor for IKK2), while resistant to TGX221 (a Keap1-Nrf2 inhibitor) and Dasatinib (a dual inhibitor for Src/Bcr-Abl), suggesting that SFXN4 might be a biomarker for drug screening (Figure 7B)."
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"IKK 16 is an inhibitor of multiple IkBa kinases (IKKs)[56] while TPCA-1 inhibits IKK2[57]."
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"IKK 16 is an inhibitor of multiple IkBa kinases (IKKs)[ xref ] while TPCA-1 inhibits IKK2[ xref ]."
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"TPCA-1 is an inhibitor of IKK2 and, thus, inhibits NF-kappaB signaling by preventing IkappaB degradation."
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"However, StA-IFN-1 and -4 (XREF_FIG, XREF_FIG) behaved as expected and were further examined by comparing their activity to the inhibitors TPCA-1, which inhibits the IFN induction pathway component IKKbeta, 15 and ruxolitinib, which inhibits IFN signaling pathway component Jak1 16 (XREF_FIG, XREF_FIG)."
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"To determine if the rapid induction of apoptosis in macrophages and DC was NF-kappaB and IKK inhibition dependent and not an off-target effect of TAT-NBD, five additional NF-kappaB inhibitory compounds were tested : Compound A (CmpA) and TPCA-1, both of which inhibit IKKbeta; MG-132, which inhibits IkappaBalpha proteosomal degradation; and IKKiVII and Wedelolactone, which inhibit both IKKalpha and IKKbeta (see XREF_SUPPLEMENTARY)."
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"Our study demonstrated [XREF_BIBR] pleiotropy for TPCA-1, which inhibited not only IKK-beta [XREF_BIBR - XREF_BIBR], but also JAK1 kinase activity [XREF_BIBR]."
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"The sustained intracellular release of TPCA-1 enabled prolonged inhibition of IKKbeta and competitively inhibited TNF-alpha from activating NF-kappaB mediated pro inflammatory cytokine secretion."
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"TPCA-1 (small molecule inhibitor of IKK-2) was employed to suppress NF-κB signaling."
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