Abnormal MEK1 activity is common in a wide range of human cancers. Identification of novel inhibitor of MEK1 is a hot subject in target specific drug discovery. Proassay MEK1 kit is a convenient, high-throughput method for enzyme-luminescence detection of MEK1 activity, which can be used for screening of Mek1 inhibitors.
The mitogen-activated protein kinase (MAPK) cascading pathways have been implicated in the regulation of diverse cellular processes such as cell proliferation, survival, differentiation, apoptosis, homeostasis and oncogenic transformation (1, 2). In normal conditions, regulation of MEK1 (mitogen-activated protein kinase kinase 1, MAP2K1, MAPKK1 or MKK1) are well-controlled by its phosphorylation and dephosphorylation by corresponding enzymes in MAPK cascading systems. However, the aberrant upregulation of MEK1 is common in a wide range of human cancers and other human disorders. The activated MEK1 will in turn phosphorylate ERK1/ERK2, the only known substrates for MEK1 at two unique sites, Thr and Tyr of the activation loop of Thr-Glu-Tyr (3). Thus, the identification of novel inhibitory molecule of MEK1 become hot subject in target specific drug discovery (3).
All kinase reactions consume ATP as a phosphate donor to phosphorylate kinase-specific substrate (4). With a luciferase-luciferin based luminescent assay platform, the amount of ATP remaining following a kinase reaction can be quantified. The “glow type” emitted light, proportional to the remaining ATP amount following kinase reaction, is inversely related to kinase activity. This luminescent system has several advantages such as non-radioactive and homogeneous, no requirement of specific antibodies, short hand-on times, cost-effective HTS assay system over other assay systems (5-7).
Kit Components • MEK1 kinase (P5055, ProteinOne) • Substrate (ERK2, P5056, ProteinOne) • assay buffer • Control inhibitor (U0126) • Detection reagent set • Deionized water • white 96-well plate (2 or 4) • User Manual
System developed for screening of MEK1 kinase inhibitors. Extensive quality control has been conducted. P9005-01 (100 assays / 96-well format) P9005-02 (200 assays / 96-well format) Please see description for details. Please see description for details.
References: 1. Davis, RJ. 1993. J Biol Chem 268:14553-14556 2. Robbins, DJ etal., 1994. Adv Cancer Res 63:93-116 3. Roberts, PJ and Der, CJ. 2007. Oncogene 26: 3291-3310 4. Curtin, M. 2005. Promega Cell Notes 13: 11-15 5. Baki A etal., 2007. Assay Drug Dev Technol 5:75-83 6. Koresawa, T and Okabe T. 2004. Assay 2:153-160 7. Klumpp, M etal., 2006. J. Biomol Screen 11:617-633
DISCLAIMER
This products is recommended For RESEARCH USE ONLY and is Not qualified for Use in Diagnostic or Therapeutic Procedures.
