NG25
Based on 24 publication(s) in Google Scholar
NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.68%
- No. CAS: 1315355-93-1
- Fòrmula: C29H30F3N5O2
- Peso molecular:537.58
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
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- Referencias
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Help & FAQs
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Immunology/Inflammation Compound Library
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Publications Citing Use of MedChemExpress (MCE) NG25
More- Nat Cell Biol. 2017 Oct;19(10):1248-1259. [Abstract]
- Cell Death Differ. 2019 Dec;26(12):2520-2534. [Abstract]
- Cell Death Dis. 2022 Apr 30;13(4):421. [Abstract]
- Int J Biol Sci. 2024 Jan 1;20(2):606-620. [Abstract]
- Proc Natl Acad Sci U S A. 2023 Dec 12;120(50):e2313148120. [Abstract]
- Oncogene. 2017 Oct 5;36(40):5620-5630. [Abstract]
- Sci Signal. 2018 Jul 10;11(538). pii: eaan5850. [Abstract]
- J Cell Biol. 2018 Aug 6;217(8):2727-2742. [Abstract]
- J Am Heart Assoc. 2021 Feb 16;10(4):e014311. [Abstract]
- Biofactors. 2020 Sep;46(5):813-820. [Abstract]
- Mol Med Rep. 2018 Jan;17(1):1710-1716. [Abstract]
- J Mol Cell Cardiol. 2021 Feb;151:31-43. [Abstract]
- Sci Rep. 2016 Sep 7;6:32737. [Abstract]
- J Cell Mol Med. 2020 Sep;24(18):10946-10957. [Abstract]
- J Immunol. 2015 Aug 1;195(3):1100-11. [Abstract]
- Biochem Biophys Res Commun. 2014 Oct 10;453(1):106-11. [Abstract]
- BMC Res Notes. 2022 Nov 26;15(1):352. [Abstract]
- Oncotarget. 2021 Oct 12;12(21):2158-2168. [Abstract]
- Universität Stuttgart. 2020 Sep.
- Norwegian University of Science and Technology. 2020 Jul.
- Oncotarget. 2017 Nov 1;8(61):104330-104346. [Abstract]
- Oncotarget. 2016 Oct 25;7(43):69173-69187. [Abstract]
- University of North Carolina. 2016.
- Harvard Medical School LINCS LIBRARY
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Ver todos los productos específicos de isoformas MAP4K
MoreVer todos los productos específicos de isoformas MAP3K
More
Actividad biológica
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MAP4K2 21.7 nM (IC50) |
TAK1 149 nM (IC50) |
LYN 12.9 nM (IC50) |
GSK 56.4 nM (IC50) |
ABL,ARG 75.2 nM (IC50) |
FER 82.3 nM (IC50) |
SRC 113 nM (IC50) |
Eph B2 672 nM (IC50) |
ZAK 698 nM (IC50) |
Eph A2 773 nM (IC50) |
Eph B4 999 nM (IC50) |
ZC1/HGK 3250 nM (IC50) |
RAF1 7590 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
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| BaF3 | IC50 |
0.018 μM
Compound: 1
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Antiproliferative activity against parental mouse BaF3 cells harbouring Bcr/Abl assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
Antiproliferative activity against parental mouse BaF3 cells harbouring Bcr/Abl assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
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[PMID: 25075558] |
| BaF3 | IC50 |
7.722 μM
Compound: 1
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Antiproliferative activity against parental mouse BaF3 cells assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
Antiproliferative activity against parental mouse BaF3 cells assessed reduction in cell viability measured after 48 hrs by Celltiter-glo assay
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[PMID: 25075558] |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 1315355-93-1
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Appearance Solid
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Peso molecular 537.58
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Fòrmula C29H30F3N5O2
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Color White to off-white
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (24)
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Journal Impact Factor
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Most Recent
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Nat Cell Biol
p38MAPK/MK2-dependent phosphorylation controls cytotoxic RIPK1 signalling in inflammation and infection. [Abstract]2017 Oct;19(10):1248-1259. PMID: 28920954
NG25 purchased from MedChemExpress. Usage Cited in: Nat Cell Biol. 2017 Oct;19(10):1248-1259. [Abstract]
Immortalized RIPK1 +/+ fetal liver mouse macrophages were infected with YopP-negative Ye-ΔyopP in presence of inhibitors for TAK1 (NP, NG25), IKKβ, IKK, p38, MK2, JNK, or MEK1/ERK. The phosphorylation of RIPK1 is analyzed by immunoblotting in cell lysates prepared after 75 min of infection.
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Cell Death Differ
TAK1 suppresses RIPK1-dependent cell death and is associated with disease progression in melanoma. [Abstract]2019 Dec;26(12):2520-2534. PMID: 30850732 -
Cell Death Dis
GCN5-mediated regulation of pathological cardiac hypertrophy via activation of the TAK1-JNK/p38 signaling pathway. [Abstract]2022 Apr 30;13(4):421. PMID: 35490166 -
Int J Biol Sci
TXNIP in liver sinusoidal endothelial cells ameliorates alcohol-associated liver disease via nitric oxide production. [Abstract]2024 Jan 1;20(2):606-620. PMID: 38169654 -
Proc Natl Acad Sci U S A
ALPK1 mutants causing ROSAH syndrome or Spiradenoma are activated by human nucleotide sugars. [Abstract]2023 Dec 12;120(50):e2313148120. PMID: 38060563 -
Oncogene
Targeting EphA2 impairs cell cycle progression and growth of basal-like/triple-negative breast cancers. [Abstract]2017 Oct 5;36(40):5620-5630. PMID: 28581527
NG25 purchased from MedChemExpress. Usage Cited in: Oncogene. 2017 Oct 5;36(40):5620-5630. [Abstract]
C3-TAg cells are starved and stimulated for 0, 15 and 30 min with ephrin-A1-Fc (EphA2 ligand; 1 μg/mL) in the presence or absence of ALW-II-41-27 or NG-25 control. EphA2 is immunoprecipitated and products probed for tyrosine phosphorylation and EphA2. ALW-II-41-27 significantly reduces basal and ephrin-A1-Fc induced tyrosine phosphorylation.
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Sci Signal
IKK promotes cytokine-induced and cancer-associated AMPK activity and attenuates phenformin-induced cell death in LKB1-deficient cells. [Abstract]2018 Jul 10;11(538). pii: eaan5850. PMID: 29991651
NG25 purchased from MedChemExpress. Usage Cited in: Sci Signal. 2018 Jul 10;11(538). pii: eaan5850. [Abstract]
A549 cells are treated for 30 min with either 5z-7-oxozeanol or NG-25 to inhibit TAK1 and immunoblotted with the indicated antibodies.
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J Cell Biol
Endosomal TLR3, TLR7, and TLR8 control neuronal morphology through different transcriptional programs. [Abstract]2018 Aug 6;217(8):2727-2742. PMID: 29777026 -
J Am Heart Assoc
2021 Feb 16;10(4):e014311. PMID: 33522247 -
Biofactors
2020 Sep;46(5):813-820. PMID: 32525617 -
Mol Med Rep
NG25, an inhibitor of transforming growth factor‑β‑activated kinase 1, ameliorates neuronal apoptosis in neonatal hypoxic‑ischemic rats. [Abstract]2018 Jan;17(1):1710-1716. PMID: 29138854
NG25 purchased from MedChemExpress. Usage Cited in: Mol Med Rep. 2018 Jan;17(1):1710-1716. [Abstract]
Expression level of p TAK1 and downstream targets following NG25 treatment. Western blot detection of p TAK1 and TAK1 expression levels in the sham group, and samples from HI, DMSO treated and NG25 treated rat brain cortexes.
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J Mol Cell Cardiol
FBXW5 acts as a negative regulator of pathological cardiac hypertrophy by decreasing the TAK1 signaling to pro-hypertrophic members of the MAPK signaling pathway. [Abstract]2021 Feb;151:31-43. PMID: 32971071 -
Sci Rep
2016 Sep 7;6:32737. PMID: 27599572
NG25 purchased from MedChemExpress. Usage Cited in: Sci Rep. 2016 Sep 7;6:32737. [Abstract]
TAK1 inhibition inhibits Dox-induced p38 activation and IκBα degradation. Breast cancer cell lines T-47D, MCF7, HCC1954, MDA-MB-231, and BT-549 are treated with Dox (20 μM) alone or combined with NG25 (2 μM) for 0, 2 h, 4 h or 6 h. The protein extracts are subjected to SDS-PAGE and immunoblotted with the antibodies against p-p38, p38, and IκBα. β-actin are detected as loading controls for whole cell extracts.
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J Cell Mol Med
Ubiquitin-specific protease 19 blunts pathological cardiac hypertrophy via inhibition of the TAK1-dependent pathway. [Abstract]2020 Sep;24(18):10946-10957. PMID: 32798288 -
J Immunol
TLR8 Senses Staphylococcus aureus RNA in Human Primary Monocytes and Macrophages and Induces IFN-β Production via a TAK1-IKKβ-IRF5 Signaling Pathway. [Abstract]2015 Aug 1;195(3):1100-11. PMID: 26085680 -
Biochem Biophys Res Commun
Identification of TGF-β-activated kinase 1 as a possible novel target for renal cell carcinoma intervention. [Abstract]2014 Oct 10;453(1):106-11. PMID: 25261726
NG25 purchased from MedChemExpress. Usage Cited in: Biochem Biophys Res Commun. 2014 Oct 10;453(1):106-11. [Abstract]
786-O/A489 RCC cells are treated with LYTAK1 (100 nM), 5Z-7-oxozeanol (5Z, 0.25 lM) or NG-25 (NG-25, 2.5 lM) for 24 h, Western blots are applied to tested list proteins.
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BMC Res Notes
2022 Nov 26;15(1):352. PMID: 36435864 -
Oncotarget
TAK1-inhibitors are cytotoxic for multiple myeloma cells alone and in combination with melphalan. [Abstract]2021 Oct 12;12(21):2158-2168. PMID: 34676048 -
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Oncotarget
EphA2 signaling is impacted by carcinoembryonic antigen cell adhesion molecule 1-L expression in colorectal cancer liver metastasis in a cell context-dependent manner. [Abstract]2017 Nov 1;8(61):104330-104346. PMID: 29262644
NG25 purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Nov 1;8(61):104330-104346. [Abstract]
MC38-CT or -CC1-L cells are treated with 1 μM of DMSO, or the non-specific NG-25 or specific ALW-II-41-27 EPHA2 receptor inhibitor for indicated periods of time, followed by stimulation with EFNA1-Fc (2 μg/mL) in the last 15 min of treatments. Protein lysates are prepared and subjected to immunoblotting using antibodies to determine the effect of kinase inhibitors on EPHA2 activation.
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Oncotarget
2016 Oct 25;7(43):69173-69187. PMID: 27732951 -
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Harvard Medical School LINCS LIBRARY
Solvente y solubilidad
DMSO : 13.46 mg/mL (25.04 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.65 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (4.65 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureza y Documentación
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Ficha de datos (282 KB)
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SDS (479 KB)
- English - EN (479 KB)
- Français - FR (479 KB)
- Deutsch - DE (479 KB)
- Norwegian - NO (479 KB)
- Español - ES (479 KB)
- Swedish - SV (479 KB)
- Italian - IT (479 KB)
- Korean - KR (479 KB)
- Portuguese - PT (479 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[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. [Content Brief]
[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. [Content Brief]
[3]. Wang Z, et al. TAK1 inhibitor NG25 enhances doxorubicin-mediated apoptosis in breast cancer cells. Sci Rep. 2016 Sep 7;6:32737. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8602 mL | 9.3009 mL | 18.6019 mL | 46.5047 mL |
| 5 mM | 0.3720 mL | 1.8602 mL | 3.7204 mL | 9.3009 mL | |
| 10 mM | 0.1860 mL | 0.9301 mL | 1.8602 mL | 4.6505 mL | |
| 15 mM | 0.1240 mL | 0.6201 mL | 1.2401 mL | 3.1003 mL | |
| 20 mM | 0.0930 mL | 0.4650 mL | 0.9301 mL | 2.3252 mL | |
| 25 mM | 0.0744 mL | 0.3720 mL | 0.7441 mL | 1.8602 mL |
NG25 Related Classifications
HY-15434 Related Classifications
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