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PD 198306

Catalog #: 2605
2 Citations Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
2605/10
PD 198306 | CAS No. 212631-61-3 | MEK Inhibitors
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Description: Selective inhibitor of MEK1/2

Chemical Name: N-(Cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-methylphenyl)amino]-benzamide

Purity: ≥98%

Product Details
Citations (2)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

PD 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.

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.
Tocris products are intended for laboratory research use only, unless stated otherwise.

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

Product Datasheets

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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

  1. Pyrrolidine dithiocarbamate activates the Nrf2 pathway in astrocytes.
    Authors: Liddell Et al.
    J Neuroinflammation  2016;13:49
  2. 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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