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)
| Quality Level | 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 |
