(5Z)-7-OXOZEAENOL
(5Z)-7-OXOZEAENOL 性质
| 熔点 | 171-173 °C(Solv: dichloromethane (75-09-2); hexane (110-54-3)) |
|---|---|
| 沸点 | 666.8±55.0 °C(Predicted) |
| 密度 | 1.270±0.06 g/cm3(Predicted) |
| 储存条件 | 2-8°C |
| 溶解度 | 二甲基亚砜：>10mg/mL |
| 形态 | 粉末 |
| 酸度系数(pKa) | 7.32±0.70(Predicted) |
| 颜色 | 白色至类白色 |
(5Z)-7-OXOZEAENOL 用途与合成方法
|
TAK1 8.1 nM (IC 50 ) |
VEGFR-2 52 nM (IC 50 ) |
VEGFR-3 110 nM (IC 50 ) |
FLT3 170 nM (IC 50 ) |
PDGFR-β 340 nM (IC 50 ) |
B-RAF VE 6300 nM (IC 50 ) |
SRC 6600 nM (IC 50 ) |
MEK1 411 nM (IC 50 ) |
5Z-7-Oxozeaenol is a potent irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 (TAK1, IC 50 , 8.1 nM), less active on MEK1 (IC 50 , 411 nM). 5Z-7-Oxozeaenol prevents inflammation by inhibiting the catalytic activity of TAK1 MAPK kinase kinase. 5Z-7-Oxozeaenol is also an inhibitor of VEGF-R2, with an IC 50 of 52 nM. 5Z-7-Oxozeaenol has inhibitory activity against VEGF-R3, FLT3, PDGFR-β, B-RAF VE and SRC, with IC 50 s of 110, 170, 340, 6300 and 6600 nM, respectively. 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.
