| Description | 5Z-7-Oxozeaenol (FR148083) is a potent, irreversible and selective inhibitor of transforming growth factor (TGF)-β-activated kinase 1 with IC50 of 8.1 nM for TAK1 and low activity against MEK1 with IC50 of 411 nM, it is also an inhibitor of VEGF-R2 with IC50 of 52 nM. |
| In vitro | 5Z-7-Oxozeaenol is a natural anti-protozoan compound from the fungal origin with inhibitory activity against VEGF-R3, FLT3, PDGFR-β, B-RAF VE, and SRC with IC50s of 110, 170, 340, 6300, and 6600 nM, respectively[1]. 5Z-7-Oxozaeenol inhibited PMA-induced AP-1 activity to almost basal levels in KT cells but had no effect on IL-1-induced NF-kB activity in KK cells[2]. 5Z-7-Oxozaeenol inhibits the JNK/p38 pathway, but it is not a direct inhibitor and is signal-specific. 5Z-7-Oxozaeenol prevents inflammation by inhibiting the catalytic activity of the TAK1 MAPK kinase[3]. |
| Target activity | FLT3:170 nM, VEGFR2:52 nM, PDGFRβ:340 nM, VEGFR3:110 nM, MEK1:411 nM, TAK1:8.1 nM, B-Raf (VE):6300 nM, Src:6600 nM |
| Synonyms | FR148083, L783279, LL-Z 1640-2 |
| molecular weight | 362.37 |
| Molecular formula | C19H22O7 |
| CAS | 253863-19-3 |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 40 mg/mL (110.38 mM), Sonication is recommended. |
| References | 1. Dakas PY, et al. Modular synthesis of radicicol A and related resorcylic acid lactones, potent kinase inhibitors. Angew Chem Int Ed Engl. 2007;46(36):6899-902. 2. Takehana K, et al. A radicicol-related macrocyclic nonaketide compound, antibiotic LL-Z1640-2, inhibits the JNK/p38 pathways in signal-specific manner. Biochem Biophys Res Commun. 1999 Apr 2;257(1):19-23. |