A natural resorcylic lactone derived from fungi that selectively inhibits purified TAK-1 (IC50 = 8.1 nM when co-expressed with the TAK-1-binding protein

(5Z)-7-Oxozeaenol – 5 mg

Brand:
Cayman
CAS:
253863-19-3
Storage:
-20
UN-No:
Non-Hazardous - /

Transforming growth factor-β-activated kinase 1 (TAK-1) is a member of the mitogen-activated protein kinase kinase kinase (MAPKKK) family that activates JNK/p38 and NF-κB pro-inflammatory signaling pathways. (5Z)-7-Oxozeaenol is a natural resorcylic lactone derived from fungi that selectively inhibits purified TAK-1 (IC50 = 8.1 nM when co-expressed with the TAK-1-binding protein) without significantly affecting the kinase activities of other MAPKKK family members (IC50 = 411 nM for MEK1).{28252} In cells, (5Z)-7-Oxozeaenol is reported to irreversibly block IL-1-induced activation of TAK-1, NF-κB, and JNK/p38 with IC50 values of 65-83 nM.{28252} (5Z)-7-Oxozeaenol has also been shown to inhibit IL-1-induced COX-2 production in cells and to relieve ear swelling induced by picryl chloride in a mouse model of COX-2-mediated inflammation.{28252} This compound has been found to sensitize cells to TRAIL- and TNF-α-induced apoptosis in vitro.{28253}  

 

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Description

A natural resorcylic lactone derived from fungi that selectively inhibits purified TAK-1 (IC50 = 8.1 nM when co-expressed with the TAK-1-binding protein, TAB1); irreversibly blocks IL-1-induced activation of TAK-1, NF-κB, and JNK/p38 (IC50s = 65-83 nM) and sensitizes cells to TRAIL- and TNF-α-induced apoptosis in vitro

Formal name: (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

Synonyms:  FR148083|L-783,279|LL-Z 1640-2

Molecular weight: 362.4

CAS: 253863-19-3

Purity: ≥99%

Formulation: A solid

Product Type|Biochemicals|Kinase Inhibitors|Other Serine/Threonine Kinases||Product Type|Biochemicals|Natural Products||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|TNF-α/NF-κB Signaling||Research Area|Immunology & Inflammation

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