A MEK inhibitor and AMPK activator
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U-0126

Item No. 70970

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2,3-bis[amino[(2-aminophenyl)thio]methylene]-butanedinitrile
CAS Number
109511-58-2
Molecular Formula
C18H16N6S2
Formula Weight
380.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF: PBS (pH 7.2)(1:2): 0.3 mg/mlDMSO: 25 mg/mlEthanol: 0.5 mg/ml
λmax
247, 308 nm
SMILES
N/C(SC1=CC=CC=C1N)=C(C#N)\C(C#N)=C(N)\SC2=C(N)C=CC=C2
InChi Code
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
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $49

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    5 mg

    $130

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    10 mg

    $236

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    25 mg

    $412

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    Product Description

    U-0126 is a MEK inhibitor with IC50 values of 72 nM and 58 nM for MEK1 and MEK2, respectively.1 It is noncompetitive with respect adenosine triphosphate (ATP) and its phosphorylation target ERK and it shows little to no inhibition against a number of other kinases including PKC, Ab1, Raf, MEKK, ERK, JNK, MKK-3, MKK-4, MKK-6, Cdk2, and Cdk4. However, U-0126 does phosphorylate and activate AMP-activated protein kinase (AMPK) in a dose-dependent manner (EC50 = 15 µM in HEK293 cells).2 It increases the ratios of ADP to ATP and AMP to ATP and increases phosphorylation of the AMPK target acetyl-CoA carboxylase (ACC).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Favata, M.F., Horiuchi, K.Y., Manos, E.J., et al. Identification of a novel inhibitor of mitogen-activated protein kinase kinase. The Journal of Biological Chemisty 273(29), 18623-18632 (1998).

    2. Dokladda, K., Green, K.A., Pan, D.A., et al. PD98059 and U0126 activate AMP-activated protein kinase by increasing the cellular AMP:ATP ratio and not via inhibition of the MAP kinase pathway. FEBS Lett. 579(1), 236-240 (2005).

    Product Citations

    West, C.E., and Silverman, N. p38b and JAK-STAT signaling protect against Invertebrate iridescent virus 6 infection in Drosophila. PLoS Pathog. 14(5):e1007020, (2018).

    Saito, Y., Chikenji, T., Ozasa, Y., et al. PDGFR signaling mediates hyperproliferation and fibrotic responses of subsynovial connective tissue cells in idiopathic carpal tunnel syndrome. Sci. Rep. 7(1), 16192 (2017).