Name: (2Z,3Z)-U0126
Rating: 5 (10 reviews)

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HIT ID:HIT212674152
Cas No:22089-22-1;218601-62-8;109511-58-2
常用名:(2Z,3Z)-U0126
IUPAC:(2Z,3Z)-bis({amino[(2-aminophenyl)sulfanyl]methylidene})butanedinitrile
IUPAC:(2Z,3Z)-bis({amino[(2-aminophenyl)sulfanyl]methylidene})butanedinitrile
InChI key:DVEXZJFMOKTQEZ-JYFOCSDGSA-N

分子式:C18H16N6S2
分子量:380.49
氢键供体数 (HBD):4
氢键受体数 (HBA):6
LogP:1.9533019
SMILES:N\C(Sc1ccccc1N)=C(\C#N)/C(/C#N)=C(\N)Sc1ccccc1N
SMILES:N\C(Sc1ccccc1N)=C(\C#N)/C(/C#N)=C(\N)Sc1ccccc1N

(2Z,3Z)-U0126 is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. It was found to functionally antagonize AP-1 transcriptional activity via noncompetitive inhibition of the dual specificity kinase MEK with IC50 of 72 nM for MEK1 and 58 nM for MEK2. U0126 inhibited anchorage-independent growth of Ki-ras-transformed rat fibroblasts by simultaneously blocking both extracellular signal-regulated kinase and mammalian target of rapamycin pathways.

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