Cat. No. 1144
Chemical Name: 1,4-Diamino-2,3-dicyano-1,4-bis[2-aminophenylthio]butadiene
Biological ActivityPotent and selective non-competitive inhibitor of MAP kinase kinase. Inhibits MEK-1 and MEK-2 (IC50 values of 0.07 and 0.06 μM respectively) with little or no effect on the activities of PKC, Abl, Raf, MEKK, ERK, JNK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 or Cdk4. Centrally active following systemic administration in vivo. Also available as part of the MAPK Cascade Inhibitor Tocriset™ and MAPK Inhibitor Tocriset™. Negative control U0124 (Cat. No. 1868) also available.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Certificate of Analysis / Safety Data Sheet
Duncia et al (1998) MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. Bioorg.Med.Chem.Lett. 8 2839. PMID: 9873633.
Favata et al (1998) Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J.Biol.Chem. 273 18623. PMID: 9660836.
Davies et al (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem.J. 351 95. PMID: 10998351.
Namura et al (2001) Intravenous administraton of MEK inhibitor U0126 affords brain protection against forebrain ischemia and focal cerebral ischemia. Proc.Natl.Acad.Sci.U.S.A. 98 11569. PMID: 11504919.
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Keywords: U0126, supplier, Potent, selective, inhibitors, MEK1, MEK2, Mitogen-Activated, Protein, Kinase, Kinases
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