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GENTAUR FRANCE

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9, Rue Lagrange • 75005 PARIS • FRANCE

U-6770 U0126, >99%

[1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)-butadiene]

 
M.W. 380.50 C18H16N6 S2

Storage:  Store at or below -20 ºC.  Solubility:  Soluble in DMSO.  Appearance:  White solid.  Disposal:  A

 

bulletSelective inhibitor of the mitogen-activated protein kinase kinases, MEK-1 and MEK-2, with 100-fold higher potency than PD 98059, but is, at most, a weak inhbitor of PKC, Raf, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, Abl, Cdk2 and Cdk4.  U0126 is an inhibitor of AP-1 transactivation in cell-based reporter assays.  Favata, M.F. et al.  "Identfication of a novel inhibitor of mitogen-activated protein kinase kinase." J. Biol. Chem. 273:  18623-18632 (1998).  DeSilva, D.R. et al.  "Inhibition of mitogen-activated protein kinase kinase blocks T cell proliferation but does not induce or prevent anergy." J. Immuol. 160:  4175-4181 (1998).  Scherle, P.A. et al.  "Inhibition of MAP kinase kinase prevents cytokine and prostaglandin E2 production in lipopolysaccharide-stimulated monocytes." J. Immuol. 161:  5681-5686 (1998).
bulletOur U0126 is highly purified.  In crystalline form and in aprotic solvents it is a single chemical entity.  However, it appears that, in solution in protic solvents, U0126 exists as a mixture of isomers.  This phenomenon does not affect overall biological activity.  Note that DMSO normally contains water so that it behaves, in this case, as a protic solvent.  (PKC Pharmaceuticals, Inc., unpublished results.)


U0126

 
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