KY-05009

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

KY-05009 在药理学上抑制人肺腺癌细胞中 TGF-β1 诱导的上皮间质转化 (EMT)。

KY-05009 pharmacologically inhibits TGF-β1-induced epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma cells. KY-05009 inhibits the protein expression of TNIK and transcriptional activity of Wnt target genes and induces apoptosis in cancer cells. KY-05009 exerts anti-cancer activity.?KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor (Ki = 100 nM).?(In Vitro):KY-05009 (1-3 μM; 48-72 hours; RPMI8226 cells) treatment induces caspase-dependent apoptosis in RPMI8226 cells in a dose-dependent manner. KY-05009 (3 μM; 1 hour; RPMI8226 cells) treatment suppresses the transcriptional activity of Wnt signaling-related genes, including TNIK, CTNNB1, TCF7, and TCF4. KY-05009 (3 μM; 9 hours; RPMI8226 cells) treatment inhibits the IL-6-induced interaction between TCF4 and β-catenin and the phosphorylation of TCF4.KY-05009 (0.1-30 μM;?24 hours;?RPMI8226 cells) treatment inhibits the proliferation of RPMI8226 cells in a dose-dependent manner.

Cell Proliferation Assay Cell Line:RPMI8226 cells Concentration:0.1 μM, 0.3 μM, 1 μM, 3 μM, 10 μM, 30 μM Incubation Time:24 hours Result:Inhibited the proliferation of RPMI8226 cells.Apoptosis Analysis Cell Line:RPMI8226 cells Concentration:1 μM, 3 μM, 10 μM Incubation Time:48 hours, 72 hours Result:Induced the binding of fluorescent Annexin V and 7-amino-actinomycin D (7-AAD) uptake.RT-PCR Cell Line:RPMI8226 cells Concentration:3 μM Incubation Time:1 hour Result:Suppressed the transcriptional activity of Wnt signaling-related genes, including TNIK, CTNNB1, TCF7, and TCF4.Western Blot Analysis Cell Line:RPMI8226 cells Concentration:3 μM Incubation Time:9 hours Result:The IL-6-induced interaction between TCF4 and β-catenin and the phosphorylation of TCF4 were inhibited.

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Wnt/Notch/Hedgehog

Wnt/beta/catenin

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1228280-29-2

352.41

C18H16N4O2S

>98% (HPLC)

In Vitro:?DMSO : 83.33 mg/mL (236.46 mM)

Cc1ccc(cc1)C(=O)Nc1sc(Nc2ccccc2)nc1C(N)=O

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(-20℃)

With Ice Pack

≥ 2 years