U0126, >99%

Catalog Number: U-6770
M.W. 380.49
C18H16N6S2
[109511-58-2]

Storage: Store at or below -20 ºC. Solubility: Soluble in DMSO at 200 mg/mL; very poorly soluble in ethanol; very poorly soluble in water; maximum solubility in plain water is estimated to be about 10-50 µM; buffers, serum, or other additives may increase or decrease the aqueous solubility. Appearance: White solid. Disposal: A.

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Thousands of labs worldwide have purchased U0126 from LC Labs (either directly from us or from our many distributors, many of whom resell under their own labels).
Selective inhibitor of the mitogen-activated protein kinase kinases, MEK-1 and MEK-2, with 100-fold higher potency than PD 98059, but is, at most, a weak inhibitor of PKC, Raf, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, Abl, Cdk2 and Cdk4. U0126 is an inhibitor of AP-1 transactivation in cell-based reporter assays. Favata, M.F., et al. "Identfication of a novel inhibitor of mitogen-activated protein kinase kinase." J. Biol. Chem. 273: 18623-18632 (1998). DeSilva, D.R., et al. "Inhibition of mitogen-activated protein kinase kinase blocks T cell proliferation but does not induce or prevent anergy." J. Immuol. 160: 4175-4181 (1998). Scherle, P.A., et al. "Inhibition of MAP kinase kinase prevents cytokine and prostaglandin E2 production in lipopolysaccharide-stimulated monocytes." J. Immuol. 161: 5681-5686 (1998).
Our U0126 is highly purified. In crystalline form and in aprotic solvents it is a single chemical entity. However, it appears that, in solution in protic solvents, U0126 exists as a mixture of isomers. This phenomenon does not affect overall biological activity. Note that DMSO normally contains water so that it behaves, in this case, as a protic solvent. (LC Laboratories, unpublished results.)
We note that U0126 is offered for sale by Sigma under the name "U0126 Ethanolate". This "ethanolate" nomenclature is somewhat ambiguous because "ethanolate" is often taken to mean "ethoxide anion" (not correct for this product) rather than "neutral ethanol included as solvent of crystallization with the primary compound" as presumably intended by Sigma. The level of solvent in our U0126 product is found on the Certificate of Analysis for each lot. Small amounts of water or other solvent of crystallization affect the molecular weight but not the biological properties of the U0126 itself.
Sold for laboratory or manufacturing purposes only; not for human, medical, veterinary, food, or household use.

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