662005

U0126

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

• Sinónimos: 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
• Fórmula empírica (notación de Hill): C₁₈H₁₆N₆S₂ · 0.5C₂H₆O
• Número CAS: 109511-58-2
• Peso molecular: 403.52
• MDL number: MFCD09971039
• UNSPSC Code: 12352200
• NACRES: NA.77
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Propiedades

• Nombre del producto: 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

Descripción

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)

Información de seguridad

• Clase de almacenamiento: 11 - Combustible Solids
• flash_point_f: Not applicable
• flash_point_c: Not applicable