|3-((1H-吡咯并[2,3-b]吡啶-4-基)氧基)-N-(4-((4-乙基哌嗪-1-基)甲基)-3-(三氟甲基)苯基)-4-甲基苯甲酰胺|CsnPharm

CAS No.: 1315355-93-1

NG25 Catalog No. CSN13920

Synonyms: NG25

NG25, a TAK1 inhibitor, inhibiting the activation of IKK by TLR7 and TLR9 agonists and preventing the secretion of type 1 IFNs induced by these ligands in Gen2.2 cells.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述NG25 is a potent TAK1 inhibitor with IC50 value of 4nM. It prevented the activation of IKKα/IKKβ and the subsequent activation of STAT1, which was due to the suppression of IFNβ secretion, at concentration of 2μM post 1-3h in Gen2.2 cells stimulated with 1μg/ml of CL097. Pre-treatment with NG25 at concentration ranging in 0.01-10μM for 1h suppressed the phosphorylation level of downstream p105, p38 and JNK1/2 stimulated by IL-1α in MEFs and human 293 IL-1R cells, and by LPS in mouse RAW cells. It also blocked signaling following stimulation of human Gen2.2 cells with the TLR7 agonist CL097. NG25 sensitizes the breast cancer cells, including T-47D, MCF7, HCC1954, MDA-MB-231 and BT-549, to Dox treatment in vitro. It partially blocked Dox-induced p38 phosphorylation and IκBα degradation and enhanced Dox-induced cytotoxic eﬀects and apoptosis in these cell lines.
作用机制NG25 may bind to the ATP binding pocket of TAK1.
参考文献

[1] Wang Z, Zhang H, et al. TAK1 inhibitor NG25 enhances doxorubicin-mediated apoptosis in breast cancer cells. Sci Rep. 2016 Sep 7;6:32737.
[2] Pauls E, Shpiro N, et al. Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cells. J Biol Chem. 2012 Jun 1;287(23):19216-28.

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
- 1.8602 mL
- 9.3010 mL
- 18.6020 mL
- 5 mM
- 0.3720 mL
- 1.8602 mL
- 3.7204 mL
- 10 mM
- 0.1860 mL
- 0.9301 mL
- 1.8602 mL

技术信息

CAS号

1315355-93-1

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C29H30F3N5O2

运输

蓝冰

分子量

537.58

别名

NG25

溶解度

DMSO	31.43 mg/mL (58.5 mM)
Water	insoluble

动物实验配方

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NG25 Catalog No. CSN13920

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