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662005

U0126

≥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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Size/SKUAvailabilityPrice
1 mg
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$109.00
5 mg
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$351.00
10 mg
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$523.00
20 mg
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$857.00

About This Item

Empirical Formula (Hill Notation):
C18H16N6S2 · 0.5C2H6O
CAS Number:
Molecular Weight:
403.52
MDL number:
UNSPSC Code:
12352200
NACRES:
NA.77
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light

$109.00


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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

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

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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This Item
662009662006U120
description

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.

description

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

description

A useful negative control for MEK inhibitors U0125 and U0126.

description

≥98% (HPLC), powder

assay

≥98% (HPLC)

assay

≥98% (HPLC)

assay

≥95% (HPLC)

assay

≥98% (HPLC)

form

solid

form

liquid

form

solid

form

powder

Quality Level

100

Quality Level

100

Quality Level

100

Quality Level

100

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

Calbiochem®

manufacturer/tradename

-

storage temp.

−20°C

storage temp.

−70°C

storage temp.

−20°C

storage temp.

2-8°C

storage condition

OK to freeze, protect from light

storage condition

OK to freeze, avoid repeated freeze/thaw cycles, desiccated (hygroscopic), protect from light

storage condition

OK to freeze, protect from light

storage condition

protect from light


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Storage Class

11 - Combustible Solids

flash_point_f

Not applicable

flash_point_c

Not applicable



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