5Z-7-Oxozeaenol

5Z-7-Oxozeaenol is a natural anti-protozoan compound from fungal origin, acting as a potent irreversible and selective inhibitor of TAK1 and VEGF-R2, with IC₅₀s of 8 nM and 52 nM, respectively. IC50 & Target:IC50: 8 nM (TAK1)^[1], 52 nM (VEGF-R2)^[2] In Vitro: 5Z-7-Oxozeaenol is a potent irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 (TAK1, IC₅₀, 8.1 nM), less active on MEK1 (IC₅₀, 411 nM). 5Z-7-Oxozeaenol prevents inflammation by inhibiting the catalytic activity of TAK1 MAPK kinase kinase^[1]. 5Z-7-Oxozeaenol is also an inhibitor of VEGF-R2, with an IC₅₀ of 52 nM. 5Z-7-Oxozeaenol has inhibitory activity against VEGF-R3, FLT3, PDGFR-β, B-RAF VE and SRC, with IC₅₀s of 110, 170, 340, 6300 and 6600 nM, respectively^[2]. 5Z-7-Oxozeaenol inhibits JNK/p38 paythway, but it is not a direct inhibitor and is signal specific. 5Z-7-Oxozeaenol suppresses the PMA-induced AP-1 activity almost to the basal level in the KT cells, but has no effects on IL-1-induced NF-kB activity in the KK cells^[3].