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Description: TGF-β-activated kinase (TAK1) inhibitor
Chemical Name: N-[4-[(4-Ethyl-1-piperazinyl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-3-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)benzamide
Purity: ≥98% (HPLC)
Biological Activity
TGF-β-activated kinase (TAK1) inhibitor (IC50 = 149 nM). Also inhibits LYN, MAP4K2 and Abl kinase activity (IC50 values are 12.9, 21.7 and 75.2 nM, respectively). Suppresses CpG A and CpG B-stimulated secretion of IFN-α and TLR7/8 agonist CL097-stimulated secretion of IFN-β in Gen 2.2 leukemia cells in vitro.
Licensing Information
Sold under license from Dana-Farber Cancer Institute.
Technical Data
| M. Wt | 537.58 |
| Formula | C29H30F3N5O2 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1315355-93-1 |
| PubChem ID | 53340664 |
| InChI Key | SMPGEBOIKULBCT-UHFFFAOYSA-N |
| Smiles | CCN1CCN(CC2=C(C(F)(F)F)C=C(NC(C3=CC(OC4=CC=NC5=C4C=CN5)=C(C)C=C3)=O)C=C2)CC1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 10.75 | 20 |
Preparing Stock Solutions
The following data is based on the product molecular weight 537.58. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 9.3 mL | 46.5 mL | 93.01 mL |
| 1 mM | 1.86 mL | 9.3 mL | 18.6 mL |
| 2 mM | 0.93 mL | 4.65 mL | 9.3 mL |
| 10 mM | 0.19 mL | 0.93 mL | 1.86 mL |
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Product Datasheets
References
References are publications that support the biological activity of the product.
Tan et al (2015) Discovery of type II inhibitors of TGFβ-activated kinase 1 (TAK1) and mitogen-activated protein kinase kinase kinase kinase 2 (MAP4K2). J.Med.Chem. 58 183 PMID: 25075558
Pauls et al (2012) Essential role for IKKβ in production of type 1 IF.s by plasmacytoid dendritic cells. J.Biol.Chem. 287 19216 PMID: 22511786
Dzamko et al (2012) The IkappaB kinase family phosphorylates the Parkinson's disease kinase LRRK2 at Ser935 and Ser910 during Toll-like receptor signaling. PLoS ONE 7 e39132 PMID: 22723946
If you know of a relevant reference for NG 25, please let us know.
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Keywords: NG 25, NG 25 supplier, NG25, TAK1, TGFbeta, TGFb, TGFβ, activated, kinases, inhibitors, inhibits, MAP4K2, LYN, Abl, Other, Kinases, 5429, Tocris Bioscience
Citations for NG 25
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Reviews for NG 25
Average Rating: 5 (Based on 1 Review.)
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Filter by:
Works for kinase assays.
By
Scott Scarneo on 02/06/2019
Assay Type: In Vitro
Species: Human
Worked in vitro Kinase assay compared to other TAK1 inhibitors.
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