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NG 25 trihydrochloride
- Parent CAS: 1315355-93-1
- Soluble in water and DMSO
- MF: C29H30F3N5O2.3HCl
- MW: 646.96
Description
NG 25 trihydrochloride is a type II kinase inhibitor of TAK1/MAP3K7 and MAP4K2/GCK with broad nanomolar activity across several kinases, including IC50 values of 149 nM for TAK1 and 22 nM for MAP4K2. It inhibits TLR7- and TLR9-induced IKKβ activation and prevents type I interferon secretion.
TAK1 and MAP4K2 link innate immune receptor activation to NF-κB, MAPK and interferon pathways. NG 25 is useful for studying kinase-dependent inflammatory signaling and type II kinase inhibitor selectivity.
Key Features
- Type II TAK1/MAP3K7 and MAP4K2 inhibitor
- IC50: 149 nM at TAK1 and 22 nM at MAP4K2
- Blocks TLR7/TLR9-induced IKKβ activation
- Suppresses type I interferon secretion in reported assays
Applications
- TAK1/MAP4K2 pharmacology
- TLR signaling studies
- NF-κB and MAPK pathway assays
- Innate immune interferon-response research
More Information
| Parent CAS No. | 1315355-93-1 |
|---|---|
| Chemical Name | 3-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide trihydrochloride |
| SMILES | C12C=CNC1=NC=CC=2OC1C(C)=CC=C(C(NC2C=C(C(F)(F)F)C(CN3CCN(CC)CC3)=CC=2)=O)C=1.Cl.Cl.Cl |
| MFCD | N.A. |
| InChi | InChI=1S/C29H30F3N5O2.3ClH/c1-3-36-12-14-37(15-13-36)18-21-6-7-22(17-24(21)29(30,31)32)35-28(38)20-5-4-19(2)26(16-20)39-25-9-11-34-27-23(25)8-10-33-27;;;/h4-11,16-17H,3,12-15,18H2,1-2H3,(H,33,34)(H,35,38);3*1H |
| InChiKey | QOIOJVPRHIAONM-UHFFFAOYSA-N |
| CID | 91826514 |
| Short Description | TAK1 (MAP3K7) and MAP4K2 inhibitor |
References
- L. Tan 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. 2014 Jul 30. [Epub ahead of print]
- E. Pauls et al. Essential role for IKKβ in production of type 1 interferons by plasmacytoid dendritic cells. J. Biol. Chem. 2012, 287, 19216-19228.
- N. Dzamko et al. The IkappaB kinase family phosphorylates the Parkinson's disease kinase LRRK2 at Ser935 and Ser910 during Toll-like receptor signaling. PLoS One. 2012, 7, e39132.
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