U0126
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U0126[1][2] is a MEK1/2 inhibitor that is used to study MEK and related signaling pathways. This inhibitor is selective for both MEK1 and MEK2,[3][4] two specific types of MEK (MAPK kinases) that are elements of the MAPK/ERK signaling pathway. This compound is usually studied in the context of cancer treatment,[5] ischemia,[6] and cellular oxidative stress.
The compound is not approved by the FDA as a therapeutic agent, and is primarily used in preclinical research settings.[7] This compound is available for research purposes from a number of companies.[8][9]
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.[10] U0126 is selective for MEK and has little to no effect on other signaling molecules such as PKC, Raf, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 and Cdk4.[11]
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.[12] 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.
Its potential for wiping long-term memories in rats has been studied at the Center for Neural Science at New York University.[13]
See also
References
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