Takinib (EDHS-206) is an orally active and selective TAK1 inhibitor (IC50=9.5 nM), more than 1.5 log more potent than the second and third ranked targets, IRAK4 (120 nM) and IRAK1 (390 nM), respectively. Takinib is an inhibitor of autophosphorylated TAK1 that non-competitively binds within the ATP binding pocket. Takinib induces apoptosis following TNFalpha stimulation in cell models of rheumatoid arthritis and metastatic breast cancer. Takinib is also a P. falciparum protein kinase 9 (PfPK9) inhibitor (KD(app) of 0.46 µM)[1][2][3].
Molecular Weight:
322.36
Purity:
99.48
CAS Number:
[1111556-37-6]
Formula:
C18H18N4O2
Target:
Apoptosis,MAP3K
Application Notes:
MCE Product type: Reference compound
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