NG25
Modify Date: 2024-02-05 08:54:11
NG25 structure
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Common Name | NG25 | ||
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| CAS Number | 1315355-93-1 | Molecular Weight | 537.57600 | |
| Density | N/A | Boiling Point | N/A | |
| Molecular Formula | C29H30F3N5O2 | Melting Point | N/A | |
| MSDS | Chinese USA | Flash Point | N/A | |
Use of NG25NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively. |
| Name | N-[4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)phenyl]-4-methyl-3-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)benzamide |
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| Synonym | More Synonyms |
| Description | NG25 is a potent dual TAK1 and MAP4K2 inhibitor, with IC50s of 149 nM and 21.7 nM, respectively. |
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| Related Catalog | |
| Target |
TAK1:149 nM (IC50) MAP4K2:21.7 nM (IC50) ZC1/HGK:3250 nM (IC50) ZAK:698 nM (IC50) RAF1:7590 nM (IC50) ABL,ARG:75.2 nM (IC50) GSK:56.4 nM (IC50) Eph A2:773 nM (IC50) Eph B2:672 nM (IC50) Eph B4:999 nM (IC50) FER:82.3 nM (IC50) LYN:12.9 nM (IC50) SRC:113 nM (IC50) |
| 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]. |
| Kinase Assay | 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 Assay | 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 |
| Molecular Formula | C29H30F3N5O2 |
|---|---|
| Molecular Weight | 537.57600 |
| Exact Mass | 537.23500 |
| PSA | 76.98000 |
| LogP | 6.33200 |
| Storage condition | 2-8℃ |
| NG25||NG-25 |
| NG25 |
| CS-0875 |
| 3-(1H-pyrrolo[2,3-b]pyridin-4-yloxy)-N-(4-((4-ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)phenyl)-4-methylbenzamide |