Description: Potent, selective inhibitor of MEK1 and 2
Chemical Name: 1,4-Diamino-2,3-dicyano-1,4-bis[2-aminophenylthio]butadiene
Biological Activity
Technical Data
Solubility
Calculators
Datasheets
References
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
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Product Datasheets
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Davieset al (2000) Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem.J. 351 95 PMID: 10998351
Dunciaet al (1998) MEK inhibitors: the chemistry and biological activity of U0126, its analogs, and cyclization products. Bioorg.Med.Chem.Lett. 8 2839 PMID: 9873633
Favataet al (1998) Identification of a novel inhibitor of mitogen-activated protein kinase kinase. J.Biol.Chem. 273 18623 PMID: 9660836
Namuraet 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
Kineharaet al (2013) Protein kinase C regulates human pluripotent stem cell self-renewal. PLoS One 8 e54122 PMID: 23349801