Chemical Name: N-(Cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-methylphenyl)amino]-benzamide
Biological ActivityPD 198306 is a potent 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.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Identification of MEK1 as a novel target for the treatment of neuropathic pain.
Ciruela et al.
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.
Pelletier et al.
Citations for PD 198306
The citations listed below are publications that use Tocris products. Selected citations for PD 198306 include:
2 Citations: Showing 1 - 2
Pyrrolidine dithiocarbamate activates the Nrf2 pathway in astrocytes.
Authors: Liddell Et al.
J Neuroinflammation 2016;13:49
Acute mitochondrial inhibition by mitogen-activated protein kinase/extracellular signal-regulated kinase kinase (MEK) 1/2 inhibitors regulates proliferation.
Authors: Ripple Et al.
J Biol Chem 2013;288:2933
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Used in vitro as ERK inhibitor in SH-SY5Y at 10 uM. Good performance.