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.