Art. -Nr.: HY-15434

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NG25

24 Cited Publications

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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.

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Reinheit: 98.68%
CAS. Nr.: 1315355-93-1
Formel: C₂₉H₃₀F₃N₅O₂
Molecular Weight:537.58

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

NG25 Chemical Structure

CAS. Nr.: 1315355-93-1

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
Chemical Information
Publications (24)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC₅₀s of 149 nM and 21.7 nM, respectively.

IC₅₀ & Target^[1]

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)

Alle MAP4K Isoform-spezifische Produkte anzeigen :

Alle MAP3K Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
BaF3	IC₅₀	0.018 μM Compound: 1	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	[PMID: 25075558]
BaF3	IC₅₀	7.722 μM Compound: 1	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	[PMID: 25075558]

In Vitro

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

CAS. Nr. 1315355-93-1
Appearance Solid
Molecular Weight 537.58
Formel C₂₉H₃₀F₃N₅O₂
Color White to off-white
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (24)

All WB

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Journal Impact Factor

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.
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
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
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
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.
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.
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

Dual-Specificity Phosphatase 26 Protects Against Cardiac Hypertrophy Through TAK1. [Abstract]

2021 Feb 16;10(4):e014311. PMID: 33522247
Biofactors

LncRNA H19 aggravates TNF-α-induced inflammatory injury via TAK1 pathway in MH7A cells. [Abstract]

2020 Sep;46(5):813-820. PMID: 32525617
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
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
Sci Rep

TAK1 inhibitor NG25 enhances doxorubicin-mediated apoptosis in breast cancer cells. [Abstract]

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.
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.
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.
BMC Res Notes

TAK1-inhibitors did not reduce disease burden in a Vκ*MYC model of multiple myeloma. [Abstract]

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
Universität Stuttgart

2020 Sep.
Norwegian University of Science and Technology

2020 Jul.
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.
Oncotarget

IKK/NF-κB signaling contributes to glioblastoma stem cell maintenance. [Abstract]

2016 Oct 25;7(43):69173-69187. PMID: 27732951
University of North Carolina

2016.
Harvard Medical School LINCS LIBRARY

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.8602 mL

9.3009 mL

18.6019 mL

5 mM

0.3720 mL

1.8602 mL

3.7204 mL

10 mM

0.1860 mL

0.9301 mL

1.8602 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.65 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Protokoll

Kinase Assay^[2]

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.

Cell Assay^[2]

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.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

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NG25

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Anti-Obesity Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) NG25

Alle MAP4K Isoform-spezifische Produkte anzeigen

Alle MAP3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NG25

Immunology/Inflammation Compound Library

Kinase Inhibitor Library

MAPK Compound Library

Anti-Cancer Compound Library

Oxygen Sensing Compound Library

Anti-Breast Cancer Compound Library

Anti-Obesity Compound Library

Human Metabolite Library

Heterocyclic Compound Library

Highly Selective Inhibitors Library

Serine/Threonine Kinase Inhibitor Library

Multi-Target Compound Library

Bioactive Compound Library Max

Kinase Inhibitor Library Mini

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) NG25

Alle MAP4K Isoform-spezifische Produkte anzeigen

Alle MAP3K Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (24)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

NG25 Related Classifications

HY-15434 Related Classifications