(5Z)-7-OXOZEAENOL
- CAS号:253863-19-3
- 英文名:LL Z1640-2
- 中文名:(5Z)-7-OXOZEAENOL
- CBNumber:CB12744545
- 分子式:C19H22O7
- 分子量:362.37
- MOL File:253863-19-3.mol
- 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 :DMSO: >10mg/mL
- 形态 :powder
- 酸度系数(pKa) :7.32±0.70(Predicted)
- 颜色 :white to off-white
(5Z)-7-OXOZEAENOL性质、用途与生产工艺
- 生物活性 5Z-7-Oxozeaneol 是一种天然的抗原生动物化合物,为有效的,不可逆的,选择性的 TAK1 和 VEGF-R2 抑制剂,IC50 值分别为 8 nM 和 52 nM。
-
靶点
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 )
-
体外研究
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.
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