Background
MEK1 and MEK2, also called MAPK or Erk kinases, are dual-specificity protein kinases that function in a mitogen activated protein kinase cascade controlling cell growth and differentiation (1-3). Activation of MEK1 and MEK2 occurs through phosphorylation of two serine residues at positions 217 and 221, located in the activation loop of subdomain VIII, by Raf-like molecules. MEK1/2 is activated by a wide variety of growth factors and cytokines and also by membrane depolarization and calcium influx (1-4). Constitutively active forms of MEK1/2 are sufficient for the transformation of NIH/3T3 cells or the differentiation of PC-12 cells (4). MEK activates p44 and p42 MAP kinase by phosphorylating both threonine and tyrosine residues at sites located within the activation loop of kinase subdomain VIII.
Molecular Formula
C18H16N6S2
Molecular Weight
380.5 g/mol
Purity
>98%
CAS
109511-58-2
Solubility
Soluble in DMSO at 35mg/ml and EtOH at 2mg/ml.
Storage
Directions for Use
U0126 has been shown to be a highly selective inhibitor of MEK 1 and MEK 2. When compared with PD98059 #9900, U0126 shows a significantly higher affinity for MEK1. U0126 and PD98059 bind to this enzyme in a mutually exclusive fashion suggesting that they share a common binding site (5). U0126 is able to inhibit both MEK1 and MEK2 while PD98059 inhibits MEK1 more potently than MEK2.
Background References
Cross-Reactivity Key
H: human M: mouse R: rat Hm: hamster Mk: monkey Vir: virus Mi: mink C: chicken Dm: D. melanogaster X: Xenopus Z: zebrafish B: bovine Dg: dog Pg: pig Sc: S. cerevisiae Ce: C. elegans Hr: horse GP: Guinea Pig Rab: rabbit All: all species expected
Trademarks and Patents
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