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Submit ReviewPD 198306
Description: Selective inhibitor of MEK1/2
Chemical Name: N-(Cyclopropylmethoxy)-3,4,5-trifluoro-2-[(4-iodo-2-methylphenyl)amino]-benzamide
Purity: ≥98% (HPLC)
Biological Activity for PD 198306
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 for PD 198306
| M. Wt | 476.23 |
| Formula | C18H16F3IN2O2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 212631-61-3 |
| PubChem ID | 9956637 |
| InChI Key | UHAXDAKQGVISBZ-UHFFFAOYSA-N |
| Smiles | CC1=C(NC2=C(C=C(F)C(F)=C2F)C(=O)NOCC2CC2)C=CC(I)=C1 |
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.
Solubility Data for PD 198306
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 47.62 | 100 | |
| ethanol | 47.62 | 100 |
Preparing Stock Solutions for PD 198306
The following data is based on the product molecular weight 476.23. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.1 mL | 10.5 mL | 21 mL |
| 5 mM | 0.42 mL | 2.1 mL | 4.2 mL |
| 10 mM | 0.21 mL | 1.05 mL | 2.1 mL |
| 50 mM | 0.04 mL | 0.21 mL | 0.42 mL |
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Product Datasheets for PD 198306
References for PD 198306
References are publications that support the biological activity of the product.
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
If you know of a relevant reference for PD 198306, please let us know.
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Keywords: PD 198306, PD 198306 supplier, Selective, inhibitors, inhibits, MEK1/2, Mitogen-Activated, Protein, Kinase, kinases, PD198306, MEK, 2605, Tocris Bioscience
2 Citations for PD 198306
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
Liddell et al (2016) Pyrrolidine dithiocarbamate activates the Nrf2 pathway in astrocytes. J Neuroinflammation 13 49 PMID: 26920699
Do you know of a great paper that uses PD 198306 from Tocris? Please let us know.
Reviews for PD 198306
Average Rating: 5 (Based on 1 Review.)
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In vitro culture.
By
Anonymous on 08/05/2018
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: SH-SY5Y
Used in vitro as ERK inhibitor in SH-SY5Y at 10 uM. Good performance.
Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
MAPK Signaling Scientific Review
MAP kinase signaling is integral to the regulation of numerous cellular processes such as proliferation and differentiation, and as a result is an important focus of cancer and immunology research. Updated for 2016, this review discusses the regulation of the MAPK pathway and properties of MAPK cascades. Compounds available from Tocris are listed.
Pathways for PD 198306
