KY-05009 是一种具有 ATP 竞争性的TNIK抑制剂，Ki为 100 nM。KY-05009 在药理上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。KY-05009 具有抗癌活性。
| 生物活性 | KY-05009 is an ATP-competitiveTraf2- and Nck-interacting kinase (TNIK)inhibitor with aKiof 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 ofTNIKand transcriptional activity ofWnttarget genes and inducesapoptosisincancercells. KY-05009 exerts anti-cancer activity[1]. |
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体外研究
(In Vitro) | KY-05009 (0.1-30 μM; 24 hours; RPMI8226 cells) treatment inhibits the proliferation of RPMI8226 cells in a dose-dependent manner[1].
KY-05009 (1-3 μM; 48-72 hours; RPMI8226 cells) treatment induces caspase-dependent apoptosis in RPMI8226 cells in a dose-dependent manner[1].
KY-05009 (3 μM; 1 hour; RPMI8226 cells) treatment suppresses the transcriptional activity of Wnt signaling-related genes, including TNIK, CTNNB1, TCF7, and TCF4[1].
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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[1].
Cell Proliferation Assay[1] | 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[1] | 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[1] | 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[1] | 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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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 83.33 mg/mL(236.46 mM;Need ultrasonic) 配制储备液 | 1 mM | 2.8376 mL | 14.1880 mL | 28.3760 mL | | 5 mM | 0.5675 mL | 2.8376 mL | 5.6752 mL | | 10 mM | 0.2838 mL | 1.4188 mL | 2.8376 mL |
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