A cell-permeable vinylogous cyanamide that acts as a selective inhibitor of MEK1/2 (IC
50 = 180 nM and 220 nM, respectively). Shown to inhibit AP-1 activity (IC
50 = 2.03 µM). Inhibits ERK1, MKK3/p38, MKK4, JNK, and PKC activities at higher concentrations (IC
50 > 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.
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Product information
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Form
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Off-white solid
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Primary Target
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MEK 1, MEK 2
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Primary Target IC50
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180 nM, 220 nM
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Secondary target
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AP-1 activity (IC50 = 2.03 µM)
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Molar mass
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335.4
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Protect from Light
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Yes
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Packaged under inert gas
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Yes
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Cell permeable
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Yes
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Purity
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≥97% by HPLC
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Solubility
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DMSO or EtOH
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Chemical formula
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C16H12F3N3S
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CAS number
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305350-87-2
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Store and ship information
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Storage
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-20°C
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Ship
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Ambient Temperature Only
Standard Handling
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