NG25
(Synonyms: N-[4-[(4-乙基-1-哌嗪基)甲基]-3-(三氟甲基)苯基]-4-甲基-3-(1H-吡咯并[2,3-B]吡啶-4-基氧基)苯甲酰胺,NG 25;NG-25) 目录号 : GC13514
An inhibitor of MAP4K2 and TAK1
Cas No.:1315355-93-1
Sample solution is provided at 25 µL, 10mM.
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NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively. NG25 also potently suppresses several kinases such as LYN, CSK, FER, p38α, ABL,ARG and SRC, with IC50s of 12.9, 56.4, 82.3, 102, 75.2, and 113 nM, respectively[1]. NG25 is very potent suppressor of CpG B- or CpG A-stimulated secretion of IFNα and CL097-stimulated secretion of IFNβ, with complete inhibition by 400 nM[2]. NG25 treatment reduces cell viability of all tested breast cancer cell lines in a dose dependent manner. NG25 (2 μM) enhances the cytotoxic effect of Dox on breast cancer cells[3].
Reference:
[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.
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Kinase experiment: |
IRF7 is expressed in Escherichia coli as a glutathione S-transferase (GST) fusion protein with a PreScission proteinase cleavage site between the GST and the IRF7. The GST-IRF7 is captured on glutathione-Sepharose and IRF7 released from GST and glutathione-Sepharose by digestion with PreScission proteinase. His6-tagged IKKβ and TBK1 are expressed in their active phosphorylated forms in insect Sf21 cells and purified by affinity chromatography on nickel nitrilotriacetate-agarose. Active GST-IKKα is purchased from Millipore and assayed. |
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Cell experiment: |
3.5×105 Gen2.2 cells or Flt3-DCs are incubated for 1 h in 96-well plates without or with the indicated concentrations of inhibitor, then stimulated with 1 μM CpG (type A or B) or 1 μg/mL of CL097 or R848. After 5 or 12 h the cell culture supernatants are collected, clarified by centrifugation, and frozen at −80°C until cytokine levels are analyzed. For cell viability assays, unstimulated cells are incubated for 12 h in the absence or presence of inhibitors. Cells are then fixed and the percentage of live cells analyzed by flow cytometry. |
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References: [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. |
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| Cas No. | 1315355-93-1 | SDF | |
| 别名 | N-[4-[(4-乙基-1-哌嗪基)甲基]-3-(三氟甲基)苯基]-4-甲基-3-(1H-吡咯并[2,3-B]吡啶-4-基氧基)苯甲酰胺,NG 25;NG-25 | ||
| 化学名 | N-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-3-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)benzamide | ||
| Canonical SMILES | CCN1CCN(CC1)CC2=C(C=C(C=C2)NC(=O)C3=CC(=C(C=C3)C)OC4=C5C=CNC5=NC=C4)C(F)(F)F | ||
| 分子式 | C29H30F3N5O2 | 分子量 | 537.58 |
| 溶解度 | Soluble in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8602 mL | 9.3009 mL | 18.6019 mL |
| 5 mM | 0.372 mL | 1.8602 mL | 3.7204 mL |
| 10 mM | 0.186 mL | 0.9301 mL | 1.8602 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet