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My CartCAS：1315355-93-1
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 1315355-93-1 |
| Name | NG25 |
| Molecular Formula | C29H30F3N5O2 |
| Molecular Weight | 537.58 |
| Solubility | Soluble in DMSO |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD19443255 |
| SMILES | O=C(NC1=CC(C(F)(F)F)=C(CN(CC2)CCN2CC)C=C1)C3=CC(OC4=C5C(NC=C5)=NC=C4)=C(C)C=C3 |
| Target Point | MAP4K |
| Passage | MAPK |
| Background | NG25 is a dual inhibitor of TAK1 and MAP4K2. |
| Biological Activity | NG25 是一种 TAK1 和 MAP4K2 的双抑制剂，IC50 值分别为 149 nM 和 21.7 nM[1-3]。 |
| IC50 | TAK1:149nM;mAP4K2:21.7nM [1-3] |
| In Vitro | NG25是一种有效的双重TAK1和MAP4K2抑制剂，IC50分别为149 nM和21.7 nM。 NG25还有效抑制几种激酶，如LYN，CSK，FER，p38α，ABL，ARG和SRC，IC50分别为12.9，56.4，82.3，102，75.2和113 nM [1]。 NG25是CpG B-或CpG A刺激的IFNα分泌和CL097刺激的IFNβ分泌的非常有效的抑制剂，完全抑制400nM [2]。 NG25处理以剂量依赖性方式降低所有测试的乳腺癌细胞系的细胞活力。 NG25(2μM)增强Dox对乳腺癌细胞的细胞毒作用[3]。 |
| Cell Experiment | 将3.5×105 Gen2.2细胞或Flt3-DC在96孔板中孵育1小时，不含或不含指定浓度的抑制剂，然后用1μMCpG(A型或B型)或1μg/ mL CL097刺激或R848。 5或12小时后，收集细胞培养物上清液，通过离心澄清，并在-80℃冷冻直至分析细胞因子水平。对于细胞活力测定，未受刺激的细胞在不存在或存在抑制剂的情况下孵育12小时。然后固定细胞并通过流式细胞术分析活细胞的百分比。 |
| Kinase Experiment | IRF7在大肠杆菌中表达为谷胱甘肽S-转移酶(GST)融合蛋白，在GST和IRF7之间具有PreScission蛋白酶切割位点。通过用PreScission蛋白酶消化，在GST和谷胱甘肽 - 琼脂糖凝胶释放的谷胱甘肽 - 琼脂糖凝胶和IRF7上捕获GST-IRF7。 His6标记的IKKβ和TBK1在昆虫Sf21细胞中以其活性磷酸化形式表达，并通过在次氮基三乙酸镍 - 琼脂糖上的亲和层析纯化。活性GST-IKKα购自Millipore并进行测定。 |
| Data Literature Source | [1]. Tan L，et al. Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J Med Chem. 2015 Jan 8;58(1):183-96. [2]. Pauls E，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. [3]. Wang Z，et al. TAK1 inhibitor NG25 enhances doxorubicin-mediated apoptosis in breast cancer cells. Sci Rep. 2016 Sep 7;6:32737 |
| Unit | Piece |
| Specification | 2mg 5mg 10mg |
NG25 是一种 TAK1 和 MAP4K2 的双抑制剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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