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(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

NG25 Chemical Structure

Cas No.:1315355-93-1

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5mg
¥2,247.00
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10mg
¥3,990.00
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500mg
¥29,400.00
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1g
¥46,200.00
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

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.

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.

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.
[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.

产品描述

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.

Chemical Properties

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
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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
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