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662005

U0126

Name: U0126
Brand: MM

≥98% (HPLC), solid, MEK inhibitor, Calbiochem^®

Synonym(s):

U0126, 1,4-Diamino-2,3-dicyano-1,4- bis(2-aminophenylthio)butadiene, MEK Inhibitor VI, 1,4-Diamino-2,3-dicyano-1,4-bis(2-aminophenylthio)butadiene, MEK Inhibitor VI

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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:

solid

Storage condition:

OK to freeze, protect from light

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Properties

Product Name

U0126, U0126, CAS 109511-58-2, is 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.

Quality Segment

100

assay

≥98% (HPLC)

form

solid

manufacturer/tradename

Calbiochem^®

storage condition

OK to freeze, protect from light

color

white

solubility

DMSO: 200 mg/mL

shipped in

ambient

storage temp.

−20°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. Shown to block doxazosin-induced osteoblastic differentiation. 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. Noncompetitive with respect to ATP. Also available in InSolution format (Cat. No. 662009).

Biochem/physiol Actions

Cell permeable: no

Primary Target
MEK1 and MEK2

Product does not compete with ATP.

Reversible: no

Target IC₅₀: 72 nM, 58 nm, against MEK1, and MEK2, respectively

Packaging

Packaged under inert gas

Preparation Note

Unstable in solution; reconstitute just prior to use.

Other Notes

Choi, Y.J., et al. 2011. Biochem. Biophys. Res. Commun.416, 232.
DeSilva, D.R., et al. 1998. J. Immunol. 160, 4175.
Duncia, J.V., et al. 1998. Biorg. Med. Chem. Lett.8, 2839.
Favata, M.F., et al. 1998. J. Biol. Chem. 273, 18623.

Legal Information

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

Disclaimer

Toxicity: Standard Handling (A)

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Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c