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662009

U0126

Name: U0126
Brand: MM

≥98% (HPLC), MEK1 inhibitor, liquid

Synonym(s):

InSolution U0126

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About This Item

Empirical Formula (Hill Notation):

C₁₈H₁₆N₆S₂ · 0.5C₂H₆O

CAS Number:

109511-58-2

Molecular Weight:

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

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Properties

Product Name

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)

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Storage Class

10 - Combustible liquids

wgk

WGK 1

flash_point_f

188.6 °F - closed cup - (Dimethylsulfoxide)

flash_point_c

87 °C - closed cup - (Dimethylsulfoxide)

Certificates of Analysis (COA)

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