5Z-7-Oxozeaenol

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

一种有效的选择性 TAK1 抑制剂，IC50 为 8 nM，选择性分别是 MEKK1 和 MEKK4 的 >33 倍和 >62 倍。

A potent, selective TAK1 inhibitor with IC50 of 8 nM, displays >33-fold and >62-fold selectivity over MEKK1 and MEKK4 respectively; inhibits IL-1-induced activation of NF-κB (IC50= 83 nM) and JNK/p38, inhibits production of inflammatory mediators, and sensitizes cells to TRAIL- and TNF-α-induced apoptosis in vitro; significantly enhances chemotherapeutic efficacy in vivo.

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. 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. 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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5Z)-7-Oxozeaenol | TAK1 inhibitor 5ZO

NF-κB

TAK1

TAK1

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253863-19-3

362.37

C19H22O7

>98% (HPLC)

DMSO : 50 mg/mL 137.98 mM

O=C(O[C@@H](C)C/C=C\1)C2=C(O)C=C(OC)C=C2/C=C/C[C@H](O)[C@H](O)C1=O

(3S,5Z,8S,9S,11E)-3,4,9,10-tetrahydro-8,9,16-trihydroxy-14-methoxy-3-methyl-1H-2-benzoxacyclotetradecin-1,7(8H)-dione

(-20℃)

With Ice Pack

≥ 2 years