Biological Activity
Potent and selective non-competitive inhibitor of MAP kinase kinase. Inhibits MEK-1 and MEK-2 (IC50 values of 0.07 and 0.06 μM respectively) with little or no effect on the activities of PKC, Abl, Raf, MEKK, ERK, JNK, MKK-3, MKK-4/SEK, MKK-6, Cdk2 or Cdk4. Brain penetrant. Helps maintain human pluripotent stem cells in undifferentiated state. Also available as part of the MAPK Cascade Inhibitor Tocriset™ and MAPK Inhibitor Tocriset™. Negative control U0124 (Cat. No. 1868) also available.
Compound Libraries
U0126 is also offered as part of the Tocriscreen Epigenetics Toolbox. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 380.48 |
| Formula | C18H16N6S2 |
| Storage | Desiccate at +4°C |
| CAS Number | 109511-58-2 |
| PubChem ID | 3006531 |
| InChI Key | DVEXZJFMOKTQEZ-JYFOCSDGSA-N |
| Smiles | NC(SC1=CC=CC=C1N)=C(C#N)/C(C#N)=C(N)SC1=CC=CC=C1N |
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.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 38.05 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 380.48. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 2.63 mL | 13.14 mL | 26.28 mL |
| 5 mM | 0.53 mL | 2.63 mL | 5.26 mL |
| 10 mM | 0.26 mL | 1.31 mL | 2.63 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.53 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Davies et al (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem.J. 351 95 PMID: 10998351
Duncia et al (1998) MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. Bioorg.Med.Chem.Lett. 8 2839 PMID: 9873633
Favata et al (1998) Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J.Biol.Chem. 273 18623 PMID: 9660836
Namura et al (2001) Intravenous administraton of MEK inhibitor U0126 affords brain protection against forebrain ischemia and focal cerebral ischemia. Proc.Natl.Acad.Sci.U.S.A. 98 11569 PMID: 11504919
Kinehara et al (2013) Protein kinase C regulates human pluripotent stem cell self-renewal. PLoS One 8 e54122 PMID: 23349801
Keywords: U0126, supplier, Potent, selective, inhibitors, inhibits, MEK1, MEK2, Mitogen-Activated, Protein, Kinase, Kinases, MEK, Stem, Cell, Proliferation, MEK, Tocris Bioscience
