Description
U0126 can inhibit MEK1 and MEK2 with IC50 of 72 nM and 58 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C20H22N6OS2
Chemical Name
(2Z,3Z)-2,3-bis(amino(2-aminophenylthio)methylene)succinonitrile,ethanol
Solubility
DMSO 85 mg/mL Water
In vitro
U0126 is noncompetitive inhibitors with respect to both MEK substrates, ATP and ERK. U0126 can inhibit MEK1 and MEK2 with IC50 of 72 nM and 58 nM. U0126 selectively repressed anchorage-independent growth of Ki-ras transformed cells. U0126 blocked not only the MAPK pathway but also the p70S6K pathway. U0126 profoundly protected HT22 cells against oxidative stress induced by glutamate, which was accompanied by an inhibition of phosphorylation of ERK1/2. U0126 also protected rat primary cultured cortical neurons against glutamate or hypoxia.
In vivo
U0126 appears to be neuroprotective in this model of hyperglycaemic ischaemic brain injury. U0126 effectively reduced the infarct size and improved neurology in hyperglycaemic rats both when given before and after ischemic onset.
Download Datasheet