CAS Number 218601-62-8 UNII 8027P94HLL 3D model (Jmol) Interactive image Pubchem 3006531 ChEMBL ID 34704 | PubChem CID 3006531 Formula C18H16N6S2 Molar mass 380.49 g/mol ChEBI ID 90693 ChemSpider ID 2276356 | |
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U0126 etoh functionally antagonizes ap 1 transcriptional activity
U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. U0126 was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-regulated kinase (ERK) and mammalian target of rapamycin (mTOR)-p70(S6K) pathways. The effects of U0126 on the growth of eight human breast cancer cell lines shown that U0126 selectively repressed anchorage-independent growth of MDA-MB231 and HBC4 cells, two lines with constitutively activated ERK. Loss of contact with substratum triggers apoptosis in many normal cell types, a phenomenon termed anoikis. U0126 sensitized MDA-MB231 and HBC4 to anoikis, i.e., upon treatment with U0126, cells deprived of anchorage entered apoptosis.
Contents
- U0126 etoh functionally antagonizes ap 1 transcriptional activity
- 2012 ford econoline wagon portsmouth nh u0126
- References
U0126 is also a weak inhibitor of PKC, Raf, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 and Cdk4.