Catalog Number: 2605
Chemical Name: N-(Cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-methylphenyl)amino]-benzamide
Biological Activity
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.
Technical Data
  • M.Wt:
    476.23
  • Formula:
    C18H16F3IN2O2
  • Solubility:
    Soluble to 100 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >98%
  • Storage:
    Store at +4°C
  • CAS No:
    212631-61-3
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.
Background References
  1. Identification of MEK1 as a novel target for the treatment of neuropathic pain.
    Ciruela et al.
    Br.J.Pharmacol., 2003;138:751
  2. 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.
    Arthrit.Rheumat., 2003;48:1582
Citations:

The citations listed below are publications that use Tocris products. Selected citations for PD 198306 include:

1 Citations: Showing 1 - 1

  1. 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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