662009

U0126

≥98% (HPLC), MEK1 inhibitor, liquid

• Synonyme(s) : InSolution U0126
• Formule empirique (notation de Hill) : C₁₈H₁₆N₆S₂ · 0.5C₂H₆O
• Numéro CAS: 109511-58-2
• Poids moléculaire : 403.52
• MDL number: MFCD09971039
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: liquid
• Storage condition: OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light

Propriétés

• Nom du produit: U0126, InSolution, ≥98%, A potent and specific inhibitor of MEK1 and MEK2
• Quality Segment: 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
• SMILES string: S(c2c(cccc2)N)\C(=C(\C(=C(\Sc1c(cccc1)N)/N)\C#N)/C#N)\N
• 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

Physical form

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

Preparation Note

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

Disclaimer

Toxicity: Irritant (B)

Informations sur la sécurité

• Classe de stockage: 10 - Combustible liquids
• Que se passe-t-il ?: WGK 1
• Point d'éclair (°F): 188.6 °F - closed cup - (Dimethylsulfoxide)
• Point d'éclair (°C): 87 °C - closed cup - (Dimethylsulfoxide)