Cat. No. 2605
Chemical Name: N-(Cyclopropylmethoxy)-3,4,5-triflu
Biological ActivityPotent inhibitor of MEK1/2. Inhibits isolated enzyme at a concentration of 8 nM and inhibits MEK activity in synovial fibroblasts at concentrations of 30 - 100 nM. Highly selective for MEK; IC50 values are > 1, > 4, > 4 and > 10 μM for ERK, c-Src, cdks and PI 3-kinase γ respectively. Antihyperalgesic; blocks static allodynia in the streptozocin model of neuropathic pain following i.t. administration.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Data Sheet
Ciruela et al (2003) Identification of MEK1 as a novel target for the treatment of neuropathic pain. Br.J.Pharmacol. 138 751. PMID: 12642375.
Pelletier et al (2003) In vivo selective inhibition of mitogen-activated protein kinase kinase 1/2 in rabbit experimental osteoarthritis is associated with a reduction in the development of structural changes. Arthrit.Rheumat. 48 1582.
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Citations are publications that use Tocris products. Selected citations for PD 198306 include:
Ripple et al (2013) Acute mitochondrial inhibition by mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK) 1/2 inhibitors regulates proliferation. J Biol Chem 288 2933. PMID: 23235157.
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Keywords: PD 198306, supplier, Selective, inhibitors, inhibits, MEK1/2, Mitogen-Activated, Protein, Kinase, kinases, PD198306, Tocris Bioscience, MEK Inhibitor products
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