Background Information: A cell-permeable vinylogous cyanamide that acts as a selective inhibitor of MEK1/2 (IC50 = 180 nM and 220 nM, respectively). Shown to inhibit AP-1 activity (IC50 = 2.03 µM). Inhibits ERK1, MKK3/p38, MKK4, JNK, and PKC activities at higher concentrations (IC50 > 10 µM). Reported to offer neuroprotection against ischemic brain injury in mice by selectively blocking ERK1/2 activation. Also suppresses IL-1β expression. Displays enhanced aqueous solubility compared to U0126 (Cat. No. 662005). Uncompetitive with respect to ATP. Supplied as a mixture of Z- and E-isomers.
Molecular Weight: 335.4
Presentation: Off-white solid. Packaged under inert gas.
Properties: Solubility: DMSO (200 mg/ml) or Ethanol (10 mg/ml).
Empirical Formula: C16H12F3N3S
Storage Conditions: Shipped at Ambient Temperature. Store at -20°C.