| 产品介绍 |
U0126-EtOH(U-0126)是MEK1和2选择性抑制剂，IC50分别为70nM和60nM，对ΔN3-S218E/S222D MEK的亲和力比PD098059强100倍。 |
| 备注 |
U0126-EtOH is a highly selective inhibitor of MEK1/2 with IC50 of 0.07 μM/0.06 μM, 100-fold higher affinity for ΔN3-S218E/S222D MEK than PD098059. |
| 生化机理 |
U0126-EtOH functionally antagonizes AP- 1 transcriptional activity and blocks the production of a variety of cytokines and metalloproteinases involved in the inflammatory response. U0126-EtOH inhibits T cell proliferation in response to antigenic stimulation or cross-linked anti-CD3 plus anti-CD28 Abs without effect on IL-2-induced proliferation by down-regulating IL-2 mRNA levels . A recent study shows that U0126-EtOH antagonizes resveratrol-induced apoptosis in castration-resistant human prostate cancer C4-2 cells, inhibits mitochondrial function and shifts cells to aerobic glycolysis independently of MEK . |
| 别名 |
U 0126;U-0126 ;2,3-双[氨基[(2-氨基苯基)硫]亚甲基]丁二腈乙醇盐;U 0126;U-0126;2,3-Bis[amino[(2-aminophenyl)thio]methylene]butanedinitrile ethanol salt |
