Pricing updated 2019-07-23. Prices are subject to change without notice.
U-0126 is a MEK inhibitor with IC50 values of 72 nM and 58 nM for MEK1 and MEK2, respectively.1 It is noncompetitive with respect adenosine triphosphate (ATP) and its phosphorylation target ERK and it shows little to no inhibition against a number of other kinases including PKC, Ab1, Raf, MEKK, ERK, JNK, MKK-3, MKK-4, MKK-6, Cdk2, and Cdk4. However, U-0126 does phosphorylate and activate AMP-activated protein kinase (AMPK) in a dose-dependent manner (EC50 = 15 µM in HEK293 cells).2 It increases the ratios of ADP to ATP and AMP to ATP and increases phosphorylation of the AMPK target acetyl-CoA carboxylase (ACC).
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Favata, M.F., Horiuchi, K.Y., Manos, E.J., et al. Identification of a novel inhibitor of mitogen-
Dokladda, K., Green, K.A., Pan, D.A., et al. PD98059 and U0126 activate AMP-
West, C.E., and Silverman, N. p38b and JAK-