Systematic (IUPAC) name | |
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1,4-diamino-2,3-dicyano-1,4-bis (2-aminophenylthio)butadiene |
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Clinical data | |
Pregnancy cat. | ? |
Legal status | ? |
Identifiers | |
ATC code | ? |
ChEMBL | CHEMBL100473 |
Chemical data | |
Formula | C18H16N6S2 |
Mol. mass | 380.49 g/mol |
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U0126, is a highly selective inhibitor of both MEK1 and MEK2, a type of MAPK/ERK kinase. U0126 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 (ERK) and mammalian target of rapamycin (mTOR)-p70(S6K) pathways. The effects of U0126 on the growth of eight human breast cancer cell lines shown that U0126 selectively repressed anchorage-independent growth of MDA-MB231 and HBC4 cells, two lines with constitutively activated ERK. Loss of contact with substratum triggers apoptosis in many normal cell types, a phenomenon termed anoikis. U0126 sensitized MDA-MB231 and HBC4 to anoikis, i.e., upon treatment with U0126, cells deprived of anchorage entered apoptosis.
U0126 is also a weak inhibitor of PKC, Raf, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 and Cdk4
It is also known to cause limited amnesia, and there seems to be some evidence that this compound could be of use for the treatment of post-traumatic stress disorder.