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CAS No. : 2503096-50-0
MCE 国际站:STAT3-IN-11
产品活性:STAT3-IN-11 (7a)是一种 STAT3 选择性抑制剂,可抑制 STAT3 pTyr705 位点的磷酸化。STAT3-IN-11 可抑制下游基因 (Survivin 和 Mcl-1) 的磷酸化,且不影响上游酪氨酸激酶 (Src and JAK2) 和 p-STAT1 的表达。STAT3-IN-11 可诱导癌细胞凋亡,有望用于 STAT3 抑制剂和抗肿瘤试剂的发现。
研究领域:JAK/STAT Signaling | Stem Cell/Wnt | Apoptosis
作用靶点:STAT | Apoptosis
In Vitro: STAT3-IN-11 (20 μM, 48 h) has 97.86% inhibitory effect on MDA-MB-231 cells.STAT3-IN-11 (0-30 μM, 48 h) inhibits several cancer cells with IC50 values of 6.01 μM (MDA-MB-231), 7.02μM (HepG2, A549), and normal human cells with IC50 values of 26.54 μM (MDA-MB-10A), 26.69 μM (PBMCs), 12.52 μM (HFL-1) .STAT3-IN-11 (2.5-10 μM, 6 h) inhibits the phosphorylation of STAT3 (stimulated by IL-6 in MDA-MB-231) at site pTyr705 in a dose-dependent manner.STAT3-IN-11 (2.5-10 μM, 6 h) inhibits the expression of the downstream gene (Survivin and Mcl-1) of STAT3 in a concentration-dependent manner.STAT3-IN-11 (2.5-10 μM, 6 h) has no effects on the typical upstream kinases of STAT3 such as p-JAK2 and p-Src and the phosphorylation of STAT1 (a STAT isoform) .STAT3-IN-11 (2.5-10 μM, 48 h) can induce cell apoptosis in a dose-manner.
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