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662009

Sigma-Aldrich

U0126

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

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Synonym(s):
InSolution U0126
Empirical Formula (Hill Notation):
C18H16N6S2 · 0.5C2H6O
CAS Number:
Molecular Weight:
403.52
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

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

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

WGK

WGK 1

Flash Point(F)

(Dimethylsulfoxide)

Flash Point(C)

(Dimethylsulfoxide)


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