产品说明书
KY-05009
 |
同义名 : | - |
| CAS号 : | 1228280-29-2 | |
| 货号 : | A168785 | |
| 分子式 : | C18H16N4O2S | |
| 纯度 : | 98+% | |
| 分子量 : | 352.41 | |
| MDL号 : | MFCD29059915 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Room temperature 液体 -20°C:3-6个月-80°C:12个月 |
|
| 溶解度 : |
DMSO: 85 mg/mL(241.2 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO |
|
| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 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 (Ki=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]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
2.84mL 0.57mL 0.28mL |
14.19mL 2.84mL 1.42mL |
28.38mL 5.68mL 2.84mL |
| 参考文献 |
|---|