KY-05009 | TNIK Inhibitor | AmBeed-信号通路专用抑制剂

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KY-05009 {[allProObj[0].p_purity_real_show]}

货号：A168785

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.

KY-05009 化学结构
CAS号：1228280-29-2

KY-05009 3D分子结构
CAS号：1228280-29-2

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KY-05009 纯度/质量文件产品仅供科研

货号：A168785 标准纯度： {[allProObj[0].p_purity_real_show]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

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KY-05009 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 (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].

KY-05009 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.

KY-05009 实验方案

计算器

存储液制备

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

KY-05009 技术信息

CAS号	1228280-29-2
分子式	C₁₈H₁₆N₄O₂S
分子量	352.41

别名
运输	蓝冰

存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

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

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计算溶液所需的质量，体积或浓度。 Ambeed 摩尔浓度计算器基于以下方程式：

浓度 (mol/L) × 体积 (L) × 分子量 (g/mol)=质量 (g)

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全球学术期刊中引用的产品

KY-05009 质控信息

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最近浏览的产品

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