KY-05009 is an ATP-competitive Traf2- and Nck-interacting kinase (TNIK) inhibitor with a K i of 100 nM. 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 In Vitro KY-05009 (0.1-30 μM; 24 hours; RPMI8226 cells) treatment inhibits the proliferation of RPMI8226 cells in a dose-dependent manner. 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Cell Proliferation AssayCell 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 AnalysisCell 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-PCRCell 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 AnalysisCell 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. Form:Solid IC50& Target:TNIK 100 nM (Ki)
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KY-05009
CAS number：1228280-29-2 molecular formula：C18H16N4O2S
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| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1228280-29-2 | molecular formula | C18H16N4O2S |
| molecular weight | 352.41 g/mol | Exact mass | ≥99% |
| PSA | 125.000 Ų | logp | 4.100 |
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