5Z-7-Oxozeaenol

SKU: orb2655745

Description

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.

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Key Properties

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CAS Number	253863-19-3
MW	362.37
Purity	>98% (HPLC)
Formula	C₁₉H₂₂O₇
SMILES	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
Target	TAK1
Solubility	DMSO : 50 mg/mL 137.98 mM

Bioactivity

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In Vitro

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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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

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TAK1

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5Z-7-Oxozeaenol (orb2655745)

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Purity:	99.00% (May vary between batches)
CAS Number:	253863-19-3
MW:	362.37
Formula:	C₁₉H₂₂O₇

5Z-7-Oxozeaenol

Description

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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