KY-05009 是 ATP 竞争性的、有效的TNIK抑制剂，Ki为 100 nM。KY-05009抑制人肺腺癌细胞中 TGF-β1 诱导的上皮-间质转化。KY-05009 还抑制TNIK的蛋白表达和Wnt靶基因的转录活性，并诱导癌细胞凋亡，显示抗癌活性。

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).

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.

1228280-29-2

C18H16N4O2S

352.41

DMSO:83.33 mg/mL (236.46 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years