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CAS No.: 1228280-29-2

KY-05009 Catalog No. CSN19765

Inhibitor of Traf2- and Nck-Interacting Kinase (TNIK; Ki value 100 nM in ATP competitive assay) that attenuates TGF-β1-mediated Wnt and Smad signaling and epithelial-to-mesenchymal transition (EMT) in human lung adenocarcinoma A549 cells. Additionally, KY05009 inhibits TGF-β1-induced phosphorylation of JNK1/2, FAK, Src, and paxillin.

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描述Serine/threonine kinase Traf2- and Nck-interacting kinase (TNIK) is a member of the germinal center kinase family that has been identified as an anti-cancer target molecule to regulate the Wnt signaling pathway. KY 05009 is a potent TNIK inhibitor with an IC50 value of 9nM. It also shows inhibitory activity against MLK1 with an IC50 value of 18nM. In serum-deprived A549 cells, incubation with KY05009 (1-10µM) for 48 h significantly inhibited TGF-β1-induced activation of the Wnt signaling pathway, but did not lead to significant cytotoxicity up to 10µM. Also in A549 cells, KY05009 at 10µM significantly inhibited TGF-β1-induced Smad2 phosphorylation and the nuclear translocation of p-Smad and Smad2/3. TGF-β1-induced migration and invasion of A549 cells were significantly inhibited by KY-05009 at 10µM^[3].
作用机制KY 05009 is a TNIK inhibitor that shows a high affinity for the ATP binding site in TNIK (K_i=100nM). There are two hydrogen bonds between KY 05009 and the Cys108 in the hinge region of TNIK. KY 05009 also has CH/π interactions with Val31, Gly111, and Leu160^[3].
参考文献

[1] Lee Y, Jung JI, et al. Synergistic inhibition effect of TNIK inhibitor KY-05009 and receptor tyrosine kinase inhibitor dovitinib on IL-6-induced proliferation and Wnt signaling pathway in human multiple myeloma cells. Oncotarget. 2017 Apr 12.
[2] Kim J, Moon SH, et al. A novel aminothiazole KY-05009 with potential to inhibit Traf2- and Nck-interacting kinase (TNIK) attenuates TGF-β1-mediated epithelial-to-mesenchymal transition in human lung adenocarcinoma A549 cells. PLoS One. 2014 Oct 22;9(10):e110180.
[3] Kim J, Moon SH, Kim BT, Chae CH, Lee JY, Kim SH. A novel aminothiazole KY-05009 with potential to inhibit Traf2- and Nck-interacting kinase (TNIK) attenuates TGF-β1-mediated epithelial-to-mesenchymal transition in human lung adenocarcinoma A549 cells. PLoS One. 2014;9(10):e110180.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 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

技术信息

CAS号

1228280-29-2

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C18H16N4O2S

运输

蓝冰

分子量

352.41

别名

溶解度

DMSO	80.0 mg/mL (227.0 mM) warming

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