662009

U0126

InSolution, ≥98%, A potent and specific inhibitor of MEK1 and MEK2

• Synonym(s): InSolution U0126
• Empirical Formula (Hill Notation): C₁₈H₁₆N₆S₂ · 0.5C₂H₆O
• CAS Number: 109511-58-2
• Molecular Weight: 403.52
• UNSPSC Code: 12352200

Properties

• Quality Level: 100
• Assay: ≥98% (HPLC)
• form: liquid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze; avoid repeated freeze/thaw cycles; desiccated (hygroscopic); protect from light
• shipped in: ambient
• storage temp.: −70°C
• InChI: 1S/C18H16N6S2/c19-9-11(17(23)25-15-7-3-1-5-13(15)21)12(10-20)18(24)26-16-8-4-2-6-14(16)22/h1-8H,21-24H2/b17-11+,18-12+
• InChI key: DVEXZJFMOKTQEZ-JYFOCSDGSA-N

Description

General description

A potent and specific inhibitor of MEK1 (IC₅₀ = 72 nM) and MEK2 (IC₅₀ = 58 nM). The inhibition is noncompetitive with respect to both ATP and ERK. Has very little effect on other kinases such as Abl, Cdk2, Cdk4, ERK, JNK, MEKK, MKK-3, MKK-4/SEK, MKK-6, PKC, and Raf. Also acts as an immunosuppressant by effectively blocking IL-2 synthesis and T cell proliferation without affecting the long-term outcomes of either T cell activation or tolerance. Reported to undergo rapid isomerization in DMSO and exist as an equilibrium mixture of (Z,Z), E,E) and (Z,E) isomers with minimal loss of activity over a period of 1 month.

Packaging

Packaged under inert gas

Warning

Toxicity: Irritant (B)

Physical form

A 100 mM (5 mg/124 µl) solution of U0126 (Cat. No. 662005) in DMSO.

Reconstitution

Following initial thaw, aliquot into precooled vials, freeze immediately at (-70°C).

Other Notes

Duncia, J.V., et al. 1998. Bioorg. Med. Chem. Lett.8, 2839.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany