Application
Takinib has been used as an inhibitor of transforming 28 growth factor - ?-activated kinase -1 (TAK-1) in human leukemia monocyticTHP-1 cells. It may be used as a TAK1 inhibitor in Jurkat cells.
Biochem/physiol Actions
Takinib is a selective inhibitor of TAK1/MAP3K7 kinase, which is a member of the MAP3K family and a key regulator of cell death. It binds in the TAk1 ATPbinding pocket with an IC50 value of 9.5 nM. Takinib selectively induced apoptosis following TNF-α stimulation in rheumatoid arthritis and breast cancer.
General description
Takinib belongs to the aminobenzimidazole class of inhibitors.
| Colour | white to beige |
|---|---|
| Manufacturer | SIGMA-ALDRICH |
| Storage Temp. | 2-8°C |
| Solubility | DMSO: 2 mg/mL, clear |
| Form | powder |
| Assay | ≥98% (HPLC) |
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