CAS号：109511-58-2
品名：1,4-二氨基-2,3-二氰基-1,4-双(邻氨基苯巯基)丁二烯(2Z,3Z)-bis{amino[(2-aminophenyl)sulfanyl]methylidene}butanedinitrile
中文别名：1,4-二氨基-2,3-二氰基-1,4-双(邻氨基苯巯基)丁二烯
英文别名：(2Z,3Z)-2,3-bis[amino-(2-aminophenyl)sulfanylmethylidene]butanedinitrile;U0126;
分子式：C18H16N6S2
分子量：380.49
精确质量：380.088
Psa：202.26
PubChem号：24278770
外观与性状：白色固体
密度：1.44 g/cm3
沸点：565.1ºC at 760 mmHg
闪点：295.6ºC
折射率：1.762
蒸汽压：8.59E-13mmHg at 25°C
简介：U0126isahighlyselectiveinhibitorofbothMEK1andMEK2,atypeofMAPK/ERKkinase.U0126wasfoundtofunctionallyantagonizeAP-1transcriptionalactivityvianoncompetitiveinhibitionofthedualspecificitykinaseMEKwithIC50of72nMforMEK1and58nMforMEK2.U0126inhibitedanchorage-independentgrowthofKi-ras-transformedratfibroblastsbysimultaneouslyblockingbothextracellularsignal-regulatedkinase(ERK)andmammaliantargetofrapamycin(mTOR)-p70(S6K)pathways.TheeffectsofU0126onthegrowthofeighthumanbreastcancercelllinesshownthatU0126selectivelyrepressedanchorage-independentgrowthofMDA-MB231andHBC4cells,twolineswithconstitutivelyactivatedERK.Lossofcontactwithsubstratumtriggersapoptosisinmanynormalcelltypes,aphenomenontermedanoikis.U0126sensitizedMDA-MB231andHBC4toanoikis,i.e.,upontreatmentwithU0126,cellsdeprivedofanchorageenteredapoptosis.
