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TPCA-1

發(fā)布日期:2017-10-26   瀏覽次數(shù):0
核心提示:a href=https://www.medchemexpress.com/TPCA-1.htmlTPCA-1/a產(chǎn)品描述:TPCA-1 is a potent inhibitor of bIKK-2/b with bICsub5
<a href="https://www.medchemexpress.com/TPCA-1.html">TPCA-1</a>產(chǎn)品描述:TPCA-1 is a potent inhibitor of <b>IKK-2</b> with <b>IC<sub>50</sub></b> of 17.9 nM.

IC50 & Target: IC50: 17.9 nM (IKK)

<i><b>In Vitro:</b></i> TPCA-1 significantly represses pro-inflammatory cytokines IL-8 and GRO-α in NPECs<sup>[1]</sup>. TPCA-1 inhibit NFκB activity as well as glioma cell proliferation and IL8 expression, and at concentrations of 2.5 and 5 μM, it blocks the TNF-induced p65 translocation into the nucleus of U87 cells<sup>[2]</sup>. TPCA-1 inhibits lipopolysaccharide-induced human monocyte production of TNF-α, IL-6, and IL-8 with an IC<sub>50</sub>=170 to 320 nM<sup>[3]</sup>.

<i><b>In Vivo:</b></i> TPCA-1 (3, 10, or 20 mg/kg, i.p.) results in a dose-dependent reduction in the severity of murine collagen-induced arthritis (CIA). TPCA-1 (10 mg/kg, i.p., b.i.d.) in vivo results in significantly decreased collagen-induced T cell proliferation ex vivo<sup>[3]</sup>. <br><br>
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