MEK1 is a protein serine/threonine kinase that is an upstream activator of the extracellular signal-regulated kinases (ERKs) which are activated in response to numerous growth factors and cytokines (1). Activation of ERKs by MEK1 involves phosphorylation of both tyrosine and threonine residues. MEK1, like the ERKs is ubiquitously distributed in tissues with the highest expression in heart, brain and spinal cord. MEK plays an important role in the growth and survival of cancer cells. In hepatocellular carcinoma, MEK activity is frequently elevated and inhibitors of MEK activity may be an effective treatment for this disease (2).
MAP2K1, MKK1, MAPKK1, PRKMK1
1. Sugden, P H. et al: Regulation of the ERK subgroup of MAP kinase cascades through G protein-coupled receptors. Cell Signal. 1997 Aug; 9(5):337-51.
2. Huynh, H. et al: Over-expression of the mitogen-activated protein kinase (MAPK) kinase (MEK)-MAPK in hepatocellular carcinoma: its role in tumor progression and apoptosis. BMC Gastroenterol. 2003 Aug 8; 3:19.
Sample Purity Data. For specific information on a given lot, see related technical data sheet.
Storage, Stability and Shipping:
Store product at –70oC. For optimal storage, aliquot target into smaller quantities after centrifugation and store at recommended temperature. For most favorable performance, avoid repeated handling and multiple freeze/thaw cycles.
Spirli Carlo et al., Cyclic AMP/PKA-dependent paradoxical activation of Raf/MEK/ERK signaling in polycystin-2 defective mice treated with sorafenib Hepatology August 2012 10.1002/hep.25872
Pan C et al., Hsp90B enhances MAST1-mediated cisplatin resistance by protecting MAST1 from proteosomal degradation The Journal of Clinical Investigations August 2019 10.1172/JCI125963
Yanga Shuping et al., Phosphorylation of KIBRA by the extracellular signal-regulated kinase (ERK)?ribosomal S6 kinase (RSK) cascade modulates cell proliferation and migration Cellular Signaling February 2014 10.1016/j.cellsig.2013.11.012
Chao; Xu, Fengrong; Niu, Yan; Wu, Yun; Sun, Jing; Peng Wang et al., Synthesis and Biological Evaluations of 3-Benzothiazol-2-yl Coumarin Derivatives as MEK1 Inhibitors Letters in Drug Design & Discovery October 2013 10.2174/15701808113109990012
Angiogenesis, Apoptosis/Autophagy, Cancer, Cardiovascular Disease, ERK/MAPK Pathway, Invasion/Metastasis, Neurobiology, Ser/Thr Kinases