253863-19-3
253863-19-3 结构式
基本信息
化合物5Z-7-OXOZEAENOL
5Z-7-OXOZE&&AELIG
LIG
NOL
L 783279
FR148083
f 152 A1
TAK1 inhibitor 5ZO)
5Z-7-Oxozeaenol >=98% (HPLC)
1H-2-Benzoxacyclotetradecin-1,7(8H)-dione, 3,4,9,10-tetrahydro-8,9,16-trihydroxy-14-methoxy-3-methyl-, (3S,5Z,8S,9S,11E)-
(2E,5S,6S,8Z,11S)-5,6,15-trihydroxy-17-methoxy-11-methyl-12-oxabicyclo[12.4.0]octadeca-1(14),2,8,15,17-pentaene-7,13-dione
物理化学性质
常见问题列表
|
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.